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【结 构 式】

【分子编号】22929

【品名】2-methoxy-1,3,2-dioxaphosphinane

【CA登记号】

【 分 子 式 】C4H9O3P

【 分 子 量 】136.087422

【元素组成】C 35.3% H 6.67% O 35.27% P 22.76%

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:(I)

The condensation of Cyclic acetonylphosphonate (II), obtained from bromoacetone and cyclic phosphite (I) by an Arbuzov reaction, with o-nitrobenzaldehyde in the presence of piperidine - AcOH salt in boiling benzene gives benzylidene phosphonale (III), which is cyclized with methyl 3-aminocrotonate (IV) in reflux in 2-propanol affording methyl 2,6-dimethyl-4-(2-nitrophenyl)-5-(2 oxo-1,3,2-dioxaphosphorinan-2-yl)-1,4 dihydro-pyridine-3 carboxylate.

1 Kimura, K.; Morita, I. (Nippon Shinyaku Co., Ltd.); 1,4-Dihydropyridine-3-carboxylate derivs.. AU 8541405; BE 0902210; EP 0159040; ES 8606276; FR 2563222; GB 2157695; JP 1985248693; US 5036059 .
2 Kimura, K.; DHP-218. Drugs Fut 1987, 12, 3, 212.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
11370 2-Nitrobenzaldehyde 552-89-6 C7H5NO3 详情 详情
20549 1-bromoacetone 598-31-2 C3H5BrO 详情 详情
(I) 22929 2-methoxy-1,3,2-dioxaphosphinane C4H9O3P 详情 详情
(II) 20572 2-(2-oxopropyl)-1,3,2lambda(5)-dioxaphosphinan-2-one C6H11O4P 详情 详情
(III) 20574 2-[(Z)-1-acetyl-2-(2-nitrophenyl)ethenyl]-1,3,2lambda(5)-dioxaphosphinan-2-one C13H14NO6P 详情 详情
Extended Information