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【结 构 式】

【分子编号】53098

【品名】Azodicarboxylic acid di-tert-butyl ester

【CA登记号】870-50-8

【 分 子 式 】C10H18N2O4

【 分 子 量 】230.264

【元素组成】C 52.16% H 7.88% N 12.17% O 27.79%

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:(XXI)

The intermediate hydrazine (XXIII) was obtained by two alternative methods. Alkylation of 4-(3-pyridyl)imidazole (II) with the chiral mesylate (XIX), prepared from (R)-1,3-butanediol (XVIII), furnished, after desilylation with tetrabutylammonium fluoride, the imidazolyl butanol (XX). Condensation of alcohol (XX) with di-tert-butyl azodicarboxylate in the presence of PPh3 yielded the hydrazine dicarboxylate (XXII), which was then deprotected to hydrazine (XXIII) under acidic conditions.

1 Kaneko, T.; McMillen, W.T.; McLaughlin, R.W.; Ripin, D.H.B.; Vanerplas, B.C. (Pfizer Inc.); Synthesis of carbamate ketolide antibiotics. EP 1088828; JP 2001151792 .
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(II) 17164 3-(1H-imidazol-4-yl)pyridine C8H7N3 详情 详情
(XVIII) 53095 (R)-(-)-1,3-Butanediol; (R)-(-)-1,3-Butylene glycol; (R)-(-)-1,3-Dihydroxybutane; (R)-1,3-Butanediol 6290-03-5 C4H10O2 详情 详情
(XIX) 53096 (1R)-3-{[tert-butyl(dimethyl)silyl]oxy}-1-methylpropyl methanesulfonate n/a C11H26O4SSi 详情 详情
(XX) 53097 (3R)-3-[4-(3-pyridinyl)-1H-imidazol-1-yl]-1-butanol n/a C12H15N3O 详情 详情
(XXI) 53098 Azodicarboxylic acid di-tert-butyl ester 870-50-8 C10H18N2O4 详情 详情
(XXII) 53099 di(tert-butyl) 1-{(3R)-3-[4-(3-pyridinyl)-1H-imidazol-1-yl]butyl}-1,2-hydrazinedicarboxylate n/a C22H33N5O4 详情 详情
(XXIII) 53100 3-{1-[(1R)-3-hydrazino-1-methylpropyl]-1H-imidazol-4-yl}pyridine n/a C12H17N5 详情 详情
Extended Information