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【结 构 式】

【分子编号】25104

【品名】N-alpha-(2,2-diphenylacetyl)-N-omega'-nitro-D-arginine

【CA登记号】

【 分 子 式 】C20H23N5O5

【 分 子 量 】413.43332

【元素组成】C 58.1% H 5.61% N 16.94% O 19.35%

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:(III)

The reaction of Nomega'-nitro-D-arginine (I) with 2,2-diphenylacetyl chloride (II) by means of NaOH in THF/water gives the expected Nalpha-diphenylacetyl derivative (III), which is condensed with 4-(ureidomethyl)benzylamine (IV) by means of TBTU and DIEA in THF to yield the corresponding amide (V). Finally, this compound is hydrogenated with H2 over Pd/C in aqueous acetic acid in order to eliminate the Nomega'-nitro group and treated with trifluoroacetic acid to provide the target compound.

1 Engel, W.; Eberlein, W.; Rudolf, K.; Doods, H.; Wieland, H.-A.; Willim, K.-D.; Entzeroth, M.; Wienen, W. (Dr. Karl Thomae GmbH); Amino acid derivs., pharmaceutical compsns. containing these cpds. and processes for preparing them. DE 19544687; EP 0885186; WO 9719911 .
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) 25103 N-omega'-nitro-D-arginine C6H13N5O4 详情 详情
(II) 23800 Diphenylacetyl chloride; 2,2-diphenylacetyl chloride 1871-76-7 C14H11ClO 详情 详情
(III) 25104 N-alpha-(2,2-diphenylacetyl)-N-omega'-nitro-D-arginine C20H23N5O5 详情 详情
(IV) 25105 N-[4-(aminomethyl)benzyl]urea C9H13N3O 详情 详情
(V) 25106 N-alpha-(2,2-diphenylacetyl)-N-omega'-nitro-N1-[4-(ureidomethyl)benzyl]-D-arginine C29H34N8O5 详情 详情
Extended Information