Research on new synthetic routes about 60166-43-0

The synthetic route of 60166-43-0 has been constantly updated, and we look forward to future research findings.

60166-43-0, name is 1,4-Dimethyl-1H-1,2,3-triazole, belongs to Triazoles compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Application In Synthesis of 1,4-Dimethyl-1H-1,2,3-triazole

A vessel containing (S)-6-(5-bromo-1-(trans-4-hydroxycyclohexyl)-1H-benzo[d]imidazol-2-yl)- 1 -(3 ,4-difluorophenyl)piperidin-2-one (intermediate 17, 50 mg,0.10 mmol), 1,4-dimethyl-1H-1,2,3-triazole (15 mg, 0.15 mmol), potassium acetate (50mg, 0.51 mmol) and tert-amyl alcohol (0.75 mL) was evacuated then backfilled withnitrogen three times. cataCXium A Pd G3 (7 mg, 10 tmol) was added and the mixturewas heated to 100 C for 18 h. The mixture was diluted with water (8 mL) then extracted with dichloromethane (3 x 8 mL). The combined organic phases were concentrated under reduced pressure to give the crude product. The crude product was purified by chromatography on silica gel (4 g column, 50-100% MeAc/isohexane) to afford a pale brown gum. The gum was triturated in tert-butyl methyl ether to yield (S)1 -(3 ,4-difluorophenyl)-6-(5-( 1 ,4-dimethyl- 1H- 1,2,3 -triazol-5-yl)- 1 -(trans-4- hydroxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one (26 mg, 0.047 mmol, 48% yield) as atan solid. LCMS (method 1): Rt 1.50 mi m/z 521 (M+H)t 1HNIVIR(DMSO-d6) 7.91 – 7.77 (m, 2H), 7.44 – 7.36 (m, 1H), 7.36 – 7.29 (m, 1H), 7.23 (dd, J= 8.5, 1.7 Hz, 1H), 7.09 -7.00 (m, 1H), 5.79 (t, J = 4.6 Hz, 1H), 4.71 (d, J = 4.1 Hz,1H), 4.41 – 4.26 (m, 1H), 3.94 (s, 3H), 3.73 – 3.61 (m, 1H), 2.55 (dt, J = 9.8, 6.2 Hz,2H), 2.48 – 2.24 (m, 2H), 2.23 (s, 3H), 2.21 – 2.12 (m, 1H), 2.08 – 1.91 (m, 3H), 1.91 -1.70 (m, 3H), 1.50- 1.35 (m, 2H), 1.25- 1.15 (m, 1H).

The synthetic route of 60166-43-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; CELLCENTRIC LTD; PEGG, Neil Anthony; TADDEI, David Michel Adrien; SHANNON, Jonathan; PAOLETTA, Silvia; QIN, Ting; HARBOTTLE, Gareth; (95 pag.)WO2018/73587; (2018); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics