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【结 构 式】

【分子编号】61408

【品名】3-Chloro-2-methylbenzenesulfonyl chloride; 3-Chloro-2-methylbenzenesulphonyl chloride

【CA登记号】80563-86-6

【 分 子 式 】C7H6Cl2O2S

【 分 子 量 】225.09484

【元素组成】C 37.35% H 2.69% Cl 31.5% O 14.22% S 14.25%

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)

Acylation of ethyl 2-amino-4-thiazolylacetate (I) with 3-chloro-2-methylbenzenesulfonyl chloride (II) in pyridine affords sulfonamide (III). After alkaline hydrolysis of the ethyl ester group of (III), the resultant carboxylic acid (IV) is coupled to N-methylpiperazine (V) by means of EDC to furnish the target amide.

1 Barf, T.; Vallgarda, J.; Emond, R.; Haggstrom, C.; Kurz, G.; Nygren, A.; Larwood, V.; Mosialou, E.; Axelsson, K.; Olsson, R.; Engblom, L.; Edling, N.; Ronquist-Nii, Y.; Ohman, B.; Alberts, P.; Abrahmsen, L.; Arylsulfonamidothiazoles as a new class of potential antidiabetic drugs. Discovery of potent and selective inhibitors of potent and selective inhibitors of the 11beta-hydroxysteroid dehydrogenase type 1. J Med Chem 2002, 45, 18, 3813.
2 Emond, R.; Barf, T.; Kurz, G.; Nilsson, M.; Vallgarda, J. (Biovitrum AB); Inhibitors of 11-beta-hydroxy steroid dehydrogenase type 1. EP 1283831; WO 0190090 .
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) 61407 Ethyl 2-amino-4-thiazoleacetate; Ethyl 2-aminothiazole-4-acetate; Ethyl-2-(2-Aminothiazole-4-Yl)acetate; (2-Amino-4-thiazolyl)acetic Acid Ethyl Ester; Ethyl (2-Amino-4-thiazolyl)acetate; Ethyl 2-(2-aminothiazol-4-yl)acetate; Ethyl 2-aminothiazol-4-yl-acetate 53266-94-7 C7H10N2O2S 详情 详情
(II) 61408 3-Chloro-2-methylbenzenesulfonyl chloride; 3-Chloro-2-methylbenzenesulphonyl chloride 80563-86-6 C7H6Cl2O2S 详情 详情
(III) 61409 ethyl 2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-4-yl)acetate C14H15ClN2O4S2 详情 详情
(IV) 61410 2-(2-{[(3-chloro-2-methylphenyl)sulfonyl]amino}-1,3-thiazol-4-yl)acetic acid C12H11ClN2O4S2 详情 详情
(V) 10061 1-Methylpiperazine; 1-Methyl piperazine; N-Methylpiperazine 109-01-3 C5H12N2 详情 详情
Extended Information