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【结 构 式】

【分子编号】31262

【品名】diethyl [bis(2-hydroxyethyl)phosphoryl](cycloheptylamino)methylphosphonate

【CA登记号】

【 分 子 式 】C16H35NO6P2

【 分 子 量 】399.404564

【元素组成】C 48.12% H 8.83% N 3.51% O 24.03% P 15.51%

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:(IV)

The reaction of cycloheptylamine (I) with triethyl orthoformate (II) and diethyl phosphite (III) at 150 gives cycloheptylaminomethylenediphosphonic acid tetraethyl ester (IV), which is then hydrolyzed with refluxing concentrated hydrochloric acid.

1 Isomura, Y.; Takeuchi, M.; Sakamoto, S.; Abe, T. (Yamanouchi Pharmaceutical Co., Ltd.); (Cycloalkylamino)methylenebisphosphonic acids and medicines containing them. AU 8928670; EP 0325482; JP 1989308290; US 5041428 .
2 Takeuchi, M.; Sakamoto, S.; Kawamuki, K.; Kudo, M.; Murase, K.; Kawashima, H.; Isomura, Y.; Synthesis and structure-activity relationships of a novel anti-resorptive agent YM175, and the related derivatives. Symp Med Chem 1990, P-12.
3 Prous, J.; Castaner, J.; YM-175. Drugs Fut 1992, 17, 4, 293.
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) 22234 cycloheptanamine; cycloheptylamine 5452-35-7 C7H15N 详情 详情
(II) 21304 Triethyl orthoformate; 1-(Diethoxymethoxy)ethane; Diethoxymethyl ethyl ether 122-51-0 C7H16O3 详情 详情
(III) 12714 diethyl phosphonate; diethyl phosphite 762-04-9 C4H11O3P 详情 详情
(IV) 31262 diethyl [bis(2-hydroxyethyl)phosphoryl](cycloheptylamino)methylphosphonate C16H35NO6P2 详情 详情
Extended Information