BIBO-3304
Chemical Name: Nalpha-(2,2-Diphenylacetyl)-D-arginine 4-(ureidomethyl)benzylamide trifluoroacetate
CAS No. 191868-14-1
项目整合开发状态: Preclinical
项目研究机构: Boehringer Ingelheim (Originator)
合成路线: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.
📌 参考资料/链接:
参考文献标题:Amino acid derivs.,pharmaceutical compsns.containing these cpds.and processes for preparing them
文献作者:Engel,W.; Eberlein,W.; Rudolf,K.; Doods,H.; Wieland,H.-A.; Willim,K.-D.; Entzeroth,M.; Wienen,W.(Dr.Karl Thomae GmbH)
参考来源:DE 19544687; EP 0885186; WO 9719911