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【结 构 式】

【分子编号】12648

【品名】2-(benzylanilino)ethyl (E)-3-amino-2-butenoate

【CA登记号】

【 分 子 式 】C19H22N2O2

【 分 子 量 】310.39596

【元素组成】C 73.52% H 7.14% N 9.03% O 10.31%

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:(VIII)

A new synthesis of efonidipine has been described: The cyclization of 2,2-dimethylbutane-1,4-diol (I) with triethyl phosphite (II) by heating at 100 C gives 2-methoxy-5,5-dimethyl-1,3,2-dioxaphosphorinan (III), which, by treatment with iodoacetone (IV) in refluxing ether, yields 2-acetonyl-5,5-dimethyl-1,3,2-dioxaphosphorinan-2-one (V). The condensation of (V) with 3-nitrobenzaldehyde (VI) by means of piperidine in acetic acid affords 3-(5,5-dimethyl-2-oxo-1,3,2-dioxaphosphorinan-2-yl)-4-(3-nitrophenyl)-3-buten-2-one (VII), which is finally cyclized with 3-amino-2-propenoic acid 2-(N-benzyl-N-phenylamino)ethyl ester (VIII) in refluxing toluene.

1 Sakoda, R.; Kamikawaji, Y.; Seto, K.; Synthesis of 1,4-dihydropyridine-5-phosphonates and their calcium antagonistic and antihypertensive activities: Novel calcium-antagonist NZ-105 and its crystal structure. Chem Pharm Bull 1992, 40, 9, 2362.
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) 12641 Neopentyl glycol; 2,2-Dimethyl-1,3-propanediol 126-30-7 C5H12O2 详情 详情
(II) 12642 Trimethyl phosphite 121-45-9 C3H9O3P 详情 详情
(III) 12643 2-Methoxy-5,5-dimethyl-1,3,2lambda(5)-dioxaphosphinan-2-one C6H13O4P 详情 详情
(IV) 12644 1-Iodoacetone C3H5IO 详情 详情
(V) 12645 5,5-Dimethyl-2-(2-oxopropyl)-1,3,2lambda(5)-dioxaphosphinan-2-one C8H15O4P 详情 详情
(VI) 12646 3-Nitrobenzaldehyde 99-61-6 C7H5NO3 详情 详情
(VII) 12647 2-[(Z)-1-Acetyl-2-(3-nitrophenyl)ethenyl]-5,5-dimethyl-1,3,2lambda(5)-dioxaphosphinan-2-one C15H18NO6P 详情 详情
(VIII) 12648 2-(benzylanilino)ethyl (E)-3-amino-2-butenoate C19H22N2O2 详情 详情
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