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【结 构 式】

【分子编号】50839

【品名】ethyl 5-amino-4-cyano-3-(2-ethoxy-2-oxoethyl)-2-thiophenecarboxylate

【CA登记号】

【 分 子 式 】C12H14N2O4S

【 分 子 量 】282.32024

【元素组成】C 51.05% H 5% N 9.92% O 22.67% S 11.36%

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)

Condensation of substituted aminothiophene (I) with ethyl bromoacetate (II) by means of K2CO3 in refluxing acetone furnishes the corresponding ethyl tetraester (III) (1), which can be converted into the desired strontium salt by treatment with NaOH in refluxing EtOH /H2O, followed by reaction with strontium hydroxide or strontium chloride in H2O. Alternatively, this transformation can also be achieved by direct treatment of (III) with strontium hydroxide in H2O/EtOH.

1 Wierzbicki, M.; et al.; Reactivity of 2-aminothiophenes. Application to the synthesis of some thieno[2,3-b]pyrroles. Bull Soc Chim France 1975, 7-8, Part 2, 1786.
2 Wierzbicki, M.; Bonnet, J.; Brisset, M.; Tsouderos, Y. (ADIR et Cie.); Bivalent metal salts of 2-N,N-di(carboxymethyl)amino, 3-cyano,4-carboxymethyl,5-carboxy-thiophene-acid, process for their preparation and pharmaceutical compsns. containing them. AU 9162033; EP 0415850; FR 2651497; JP 1991169876; US 5128367 .
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) 50839 ethyl 5-amino-4-cyano-3-(2-ethoxy-2-oxoethyl)-2-thiophenecarboxylate C12H14N2O4S 详情 详情
(II) 16640 Ethyl 2-bromoacetate; Ethyl bromoacetate 105-36-2 C4H7BrO2 详情 详情
(III) 50840 ethyl 5-[bis(2-ethoxy-2-oxoethyl)amino]-4-cyano-3-(2-ethoxy-2-oxoethyl)-2-thiophenecarboxylate C20H26N2O8S 详情 详情
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