Tag: M.W=300-400

Synthetic Route of 31250-99-4, New Advances in Chemical Research in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 31250-99-4, name is 1-Trityl-1H-1,2,4-triazole, molecular formula is C21H17N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

a) A solution of 1-trityl-1,2,4-triazole (10.0 g, prepared as described in Example 1) and N,N,N’,N’-tetramethylethylenediamine (3.8 g) in dry tetrahydrofuran (250 ml) was cooled to -70 C. under nitrogen. n-Butyllithium (22.2 ml, 1.6M solution in hexane) was added dropwise, with stirring, at such a rate that the internal temperature was maintained below -60 C. The red solution was stirred at -70 C. for twenty-five minutes, then treated dropwise with diethyl 3-oxo-propane phosphonate (6.20 g, prepared by formic acid deacetalisation of the diethyl acetal, DE 2517448, and also described in, for example, Tetrahedron 1981, 37, 1377) whilst maintaining the temperature at that level. The mixture was stirred for two and a half hours at -70 C. then quenched, at that temperature, with saturated aqueous ammonium chloride solution. It was extracted with ethyl acetate and the organic phase washed with brine, dried over magnesium sulphate, and evaporated under reduced pressure to give crude diethyl 3-hydroxy-3(1-trityl-1,2,4-triazol-5-yl)propane phosphonate (10.81 g). Chromatography on silica, using dichloromethane-ethanol (19:1) as eluant, gave pure material, m.p. 154-155 C. NMR (CDCl3): delta1.3(6H,t), 1.9(2H,m), 1.7(2H,m), 3.1(1H,br), 4.0(4H,m), 4.1(1H,t), 7.1-7.3 (15H,m), 7.9(1H,s). M/S: M+ 505.

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Reference:
Patent; Zeneca Limited; US5393732; (1995); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 107534-96-3, New discoveries in chemical research and development in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 107534-96-3, name is 3-((1H-1,2,4-Triazol-1-yl)methyl)-1-(4-chlorophenyl)-4,4-dimethylpentan-3-ol, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

EXAMPLE 2 Preparation of 1-Tert-butyl-3-(p-chlorophenyl)-1-(1H-1,2,4-triazol-1-ylmethyl)propyl diphenylborinate STR11 A solution of diphenylborinic acid (0.11 g, 0.60 mmol) in toluene is added to a solution of 1-(4-chlorophenyl)-4,4-dimethyl-3-(1H-1,2,4-triazol-1-ylmethyl)pentan-3-ol (0.21 g, 0.68 mmol) in a 1:1 ether/toluene solution. The reaction mixture is heated at reflux for 3 days with removal of water (Dean Stark), cooled and concentrated in vacuo to obtain a residue. The residue is chromatographed using silica gel and hexane/ethyl acetate solutions to give the title product as a pale yellow solid, mp 197 C.

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Reference:
Patent; American Cyanamid Company; US5591726; (1997); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Synthetic Route of 1533519-85-5, New Advances in Chemical Research in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 1533519-85-5, name is Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate, molecular formula is C18H17N3O2S, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

32 g of methyl 2-(4-(4-cyclopropyl-1-naphthyl)-4hydro-1,2,4-triazol-3-ylsulfanyl)acetate are placedIn a 10L flask, 600 mL of acetonitrile and 20 mL of pyridine were added, and the mixture was stirred and dissolved. After the solution was completely dissolved, the mixture was dropped at a rate of 10 mL/min.90mL of a 1mol/L Bromine Br2-acetonitrile solution was added dropwise at room temperature for 2 hours. After the reaction was complete, 2L of B was added to the reaction.Ethyl acetate was dissolved, washed twice with saturated brine, and washed with 1 L each time. The organic phase was collected and dried over saturated sodium sulfate.Concentrate and filter to obtain methyl 2-(5-bromo-4-(4-cyclopropyl-1-naphthyl)-4hydro-1,2,4triazol-3-ylsulfanyl)acetate.34.5 g, yield 87.3%; purity 98.2%.

I am very proud of our efforts over the past few months and hope to Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate help many people in the next few years.

Reference:
Patent; Chengdu Meiyugao Pharmaceutical Co., Ltd.; Wang Chunyan; Chen Zhiyong; Sui Yumin; (17 pag.)CN107955029; (2018); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 1533519-85-5, New discoveries in chemical research and development in 2021. We’ll be discussing some of the latest developments in chemical about CAS: 1533519-85-5, name is Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.

Take 8.0g of the purified product of compound (4) obtained in Example 3, 64ml of tetrahydrofuran, start stirring, warm up to T=30~35C, stir until dissolved; add 6.4g NBS, stir the reaction for 3~4h, the reaction is completed, and the temperature is reduced to T 05, add 40ml of toluene, add 40ml of purified water dropwise, the temperature is controlled not to exceed 7, drop it, stir for 10min, let stand for liquid separation; the organic phase is cooled to 05, add 3% hydrogen sulfite dropwise 40ml of sodium solution, keep the temperature below 10C, drop after completion, stir for 20min, stand for liquid separation, collect organic phase; warm to 1825C with camera, add 40ml of 7% sodium bicarbonate solution, stir for 10min, stand for liquid separation , Collect the organic phase, concentrate and dry to prepare the Recinade product, and test its purity to 99.940%.

The potential utility of systematic synthetic strategy will be applicable to efficient generations of chemical libraries of compounds to find ‘hit’ molecules.Read on for other articles about Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate, hurry up and to see.

Reference:
Patent; Beijing Xinkaiyuan Pharmaceutical Technology Co., Ltd. Hainan Fen Corporation; Xia Zhongning; Wu Jin; Wang Shiwei; (10 pag.)CN111116500; (2020); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

New discoveries in chemical research and development in 2021. The transformation of simple hydrocarbons into more complex and valuable products via catalytic C–H bond functionalisation has revolutionised modern synthetic chemistry. 1533519-85-5, name is Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Safety of Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate

250mL was added to the reaction flask the product of step B (4g, 0.0118mol), tetrahydrofuran (30ml), tetramethylpiperidinePyridine (TEMPO, 0.2g, 0.1eq), an oil bath at 30 ~ 32 heating and stirring to dissolve until clear. Portionwise added N- bromosuccinimideImide (NBS, 3.2g, 0.018mol, 1.5eq), temperature does not exceed 35 . Plus complete, insulation 30 ~ 32 reaction 3h.Sample testing of raw materials after the reaction was complete, heating was stopped, the ice bath to cool. Until an internal temperature of 0 ~ 5 , water portionwise sodium sulfiteThe reaction was quenched solution was extracted with ethyl acetate, dried over anhydrous sodium sulfate, filtration, spin dry, and the resulting crude intermediate C directlyUsed in the next reaction.Samples were analyzed by column chromatography (200-300 mesh silica gel, eluting with methylene chloride: methanol = 15: 1) to giveWhite solid C.

I hope this article can help some friends in scientific research. I am very proud of our efforts over the past few months and hope to Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate help many people in the next few years.

Reference:
Patent; Zhejiang Jingxin Pharmaceutical Co., Ltd.; Huang, yue; Xu, hui; Zhangyu, bin; Zheng, fei; (19 pag.)CN105399694; (2016); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 1533519-85-5, New Advances in Chemical Research in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic,A common heterocyclic compound, 1533519-85-5, name is Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate, molecular formula is C18H17N3O2S, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

Example 11. Preparation of methyl 2-((5-bromo-4-(4-cyclopropylnaphthalen-l-yl)-4H-l,2,4-triazol-3-yl)thio)acetate [076] To a flask added methyl 2-((4-(4-cyclopropylnaphthalen-l-yl)-4H-l,2,4-triazol-3-yl)thio)acetate (4.0 g, 11.8 mmol), l,3-Dibromo-5,5-dimethylhydantoin (11.8 mmol) and ethyl acetate (100 mL) to form a mixture, the mixture was heated to reflux, after the reaction was complete, the mixture was cooled to room temperature, then worked up to obtain phenyl 2-((5-bromo-4-(4-cyclopropylnaphthalen-l-yl)-4H-l,2,4-triazol-3-yl)thio)acetate as a yellow solid 4.9 g, yield 99%, LC-Ms: m/z (ESI): 418,420 (M+H)+, 1H NMR (400 MHz, CDC13): delta 8.57 (d, J=8.0 Hz, 1 H), 7.69 (m, 1 H), 7.61 (m, 1 H), 7.39 (s, 2 H), 7.26 (d, J=8.4 Hz, 1 H), 4.07 (dd, J=16.0, 25.6 Hz, 2 H), 3.75 (s, 3 H), 2.46 (m, 1 H), 1.20 (m, 2 H), 0.91 (m, 2 H).

By the way, if you are interested in learning more fun chemistry with your kids, get your hands into one chemistry set now, and start enjoying the best part of chemistry: experiments about Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate.

Reference:
Patent; SUNSHINE LAKE PHARMA CO., LTD.; CHEN, Weiqiang; LUO, Jian; LIU, Lixue; FAN, Yuping; WO2014/198241; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

New discoveries in chemical research and development in 2021. The dynamic chemical diversity of the numerous elements, ions and molecules that constitute the basis of life provides wide challenges and opportunities for research. 107534-96-3, name is 3-((1H-1,2,4-Triazol-1-yl)methyl)-1-(4-chlorophenyl)-4,4-dimethylpentan-3-ol belongs to triazoles compound, it is a common compound, a new synthetic route is introduced below. Quality Control of 3-((1H-1,2,4-Triazol-1-yl)methyl)-1-(4-chlorophenyl)-4,4-dimethylpentan-3-ol

For a 1 :1 co-crystal of tebuconazol and 4-hydroxy benzoic acid, 200,1 mg of tebucona- zol, 80,4 mg of 4-hydroxi benzoic acid and 150 muIota ethanol was grinded in a ball mill (Retsch Modell MM301 ) for 10 minutes by using 20 Hz. The crystalline product gave the PXRD in Figure 3 (table 5).

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Reference:
Patent; BASF SE; SAXELL, Heidi, Emilia; ISRAELS, Rafel; SCHAeFER, Ansgar; BRATZ, Matthias; HOeFFKEN, Hans, Wolfgang; BRODE, Ingo; NAUHA, Elisa; NISSINEN, Maija; WO2011/54741; (2011); A2;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Reference of 107534-96-3, New Advances in Chemical Research in 2021. Chemo-enzymatic cascade processes are invaluable due to their ability to rapidly construct high-value products from available feedstock chemicals in a one-pot relay manner. 107534-96-3, name is 3-((1H-1,2,4-Triazol-1-yl)methyl)-1-(4-chlorophenyl)-4,4-dimethylpentan-3-ol, molecular formula is C16H22ClN3O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

A portion of cis-[PtCl2(DMSO)2] (0.53 g, 1.26 mmol) placed into a pear-shaped flask of 100 mL in volume was dissolved in chloroform (20 mL) under stirring on a water bath (40C). To the resulting solution, reagent L (0.89 g, 2.89 mmol) was added. The formed light-yellow transparent solution was boiled on a water bath for 19 h under reflux and magnetically stirring and then transferred into a 150-mL beaker and evaporated one-half. Complex I was precipitated from the solution cooled to room temperature with hexane. The mixture of the precipitate and the mother solution was cooled to 10C, the solution was then decanted, and hexane (100 mL) was added to the precipitate, thereupon the mixture was allowed to stand at -10C for 15 h. The precipitate was twice washed with hexane, reprecipitated with hexane from a chloroform solution, filtered out, washed with hexane, and dried in air. The yield was 62%.

I am very proud of our efforts over the past few months and hope to 3-((1H-1,2,4-Triazol-1-yl)methyl)-1-(4-chlorophenyl)-4,4-dimethylpentan-3-ol help many people in the next few years.

Reference:
Article; Khisamutdinov; Anpilogova; Shitikova; Murinov, Yu. I.; Russian Journal of Inorganic Chemistry; vol. 61; 12; (2016); p. 1530 – 1537; Zh. Neorg. Khim.; vol. 61; 12; (2016); p. 1591 – 1598,8;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 31250-99-4, New Advances in Chemical Research in 2021. Redox catalysis has been broadly utilized in electrochemical synthesis due to its kinetic advantages over direct electrolysis. 31250-99-4, name is 1-Trityl-1H-1,2,4-triazole, molecular formula is C21H17N3, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

Triethylamine (5.49 g, 54.30 mmol) is added to a solution of 1,2,4-triazole (3.0 g, 43.44 mmol) in DMF (50 mL) at rt. After stirring for 5 minutes, trityl chloride (12.11 g, 43.44 mmol) is added as a solid and the mixture is stirred overnight. The solvent is distilled off under reduced pressure and the crude is partitioned between dichloromethane (50 mL) and water (50 mL). The organic layer is separated and the aqueous layer is extracted with dichloromethane (3 x 50 mL). The combined organic layers are washed with water (3 x 40 mL). The organic layer is dried over Na2SO4 and concentrated under reduced pressure to afford the product 1-trytil-1H- 1,2,4-triazole (12.6 g, 93 %). n-BuLi (4.5 mL, 11.24 mmol; 2.5 M solution in hexanes) is added to a solution of 1-trityl-1H-1,2,4-triazole (3.5 g, 11.24 mmol) in THF (120 mL) at -78C and the solution is stirred for 45 mm. Bromine (1.76 g, 11.02 mmol) is added dropwise over a period of 5 minutes and the solution is stirred for 2 h allowed to warm to -20 C and quenched by adding saturated NH4C1 solution (30 mL). The reaction mixture ias diluted with water (60 mL) and dichloromethane (40 mL). The organic layer is separated and the aqueous layer is extracted with CH2C12 (4 x 50 mL).The combined organic extract was dried over Na2SO4 and the solvent evaporated under reduced pressure to afford crude which is used as such for the next step (4.2 g, 95 %). 7.09-7.16 (m, 6H), 7.27-7.40 (m, 9H), 7.86 (s, 1H).

I am very proud of our efforts over the past few months and hope to 1-Trityl-1H-1,2,4-triazole help many people in the next few years.

Reference:
Patent; NEWLINK GENETICS CORPORATION; KUMAR, Sanjeev; WALDO, Jesse; JAIPURI, Firoz; MAUTINO, Mario; WO2014/159248; (2014); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics

Application of 1533519-85-5, New Advances in Chemical Research in 2021. The prevalence of solvent effects in heterogeneous catalysis in condensed media has motivated developing quantitative kinetic,A common heterocyclic compound, 1533519-85-5, name is Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate, molecular formula is C18H17N3O2S, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, below Introduce a new synthetic route.

Into a 1L three-necked flask, add 20.0g of intermediate (4), 80ml of tetrahydrofuran and 20ml of methanol, start stirring, warm up to 40.0C, stir until dissolved; add 20.0g NBS, 0.2g TEMPO, react for 60min; cool to 5C, add ethyl acetate 100ml and purified water 120ml, the organic phase was washed with 120ml of 3% sodium bisulfite solution and 100ml of 5% sodium bicarbonate solution, dried with anhydrous sodium sulfate 50.0g, filtered, rinsed with ethyl acetate 50ml, the mother liquor was concentrated to dryness, 60ml of ethyl acetate was added to the residue, heated until the solid was dissolved, 240ml of n-hexane was added, and the temperature was slowly lowered to 0-5C, filtered, washed, and dried to obtain 22.0g of off-white solid with a yield of 89.4%.

By the way, if you are interested in learning more fun chemistry with your kids, get your hands into one chemistry set now, and start enjoying the best part of chemistry: experiments about Methyl 2-((4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-yl)thio)acetate.

Reference:
Patent; Beijing Xinkaiyuan Pharmaceutical Technology Co., Ltd. Hainan Fen Corporation; Xia Zhongning; Wu Jin; Bai Bingxin; (9 pag.)CN111116501; (2020); A;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics