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【结 构 式】

【分子编号】62817

【品名】3-(chloromethyl)-1,2,4,5-tetramethylbenzene

【CA登记号】

【 分 子 式 】C11H15Cl

【 分 子 量 】182.6928

【元素组成】C 72.32% H 8.28% Cl 19.41%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(II)

Alkylation of the sodium salt of indole-4-carbaldehyde (I) with 2,3,5,6-tetramethylbenzyl chloride (II) affords the N-alkylated indole aldehyde (III). Subsequent condensation of aldehyde (III) with 3-cyano-4-hydroxybenzoic acid hydrazide (IV) in DMSO in the presence of an acidic catalyst yields the target acyl hydrazone.

1 Madsen, P.; Ling, A.; Plewe, M.; et al.; Optimization of alkylidene hydrazide based human glucagon receptor antagonists. Discovery of the highly potent orally available 3-cyano-4-hydroxybenzoic acid [1-(2,3,5,6-tetramethylbenzyl)-1H-indol-4-ylmethylene]hydrazide. J Med Chem 2002, 45, 26, 5755.
2 Lau, J.; Madsen, P.; Truesdale, L.K.; Sams, C.; Feng, J.; Kiel, D.; Ling, A.; Kukl, A.; Shi, S.; Plewe, M.B.; May, J. (Agouron Pharmaceuticals, Inc.; Novo Nordisk A/S); Glucagon antagonists/inverse agonists. JP 2002533439; WO 0039088 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 62816 1H-indole-4-carbaldehyde C9H7NO 详情 详情
(II) 62817 3-(chloromethyl)-1,2,4,5-tetramethylbenzene C11H15Cl 详情 详情
(III) 62818 1-(2,3,5,6-tetramethylbenzyl)-1H-indole-4-carbaldehyde C20H21NO 详情 详情
(IV) 60848 3-cyano-4-hydroxybenzohydrazide C8H7N3O2 详情 详情
Extended Information