ICI-155387, CB-3717-药物合成数据库

【药物名称】ICI-155387, CB-3717

化学结构式(Chemical Structure):

参考文献No.	75194
标题:	CB-3717
作者:	Hopkins, S.J.; Serradell, M.N.; Casta馿r, J.
来源:	Drugs Fut 1984,9(12),893

合成路线图解说明: The alkylation of diethyl N-(4-aminobenzoyl)glutamate (I) with propargyl bromide (II) in hot ethanol gives diethyl N-[4-(propargylamino)benzoyl]glutamate (III), which is condensed with 2-amino-6-bromomethyl-4-hydroxyquinazoline (IV) by means of triethylamine in hot 2-ethoxyethanol (or CaCO3 in dimethylacetamide) yielding diethyl N-[4-[N-[(2-amino-4-hydroxy-6-quinazolinyl)methyl]prop-2-ynylamino]benzoyl]-L-glutamate (V). Finally, this compound is saponified with NaOH in ethanol-water.

参考文献No.	701195
标题:	Anti-cancer quinazoline derivatives
作者:	Jones, T.R.; Harrap, K.R.; Calvert, A.H.
来源:	EP 0031237; GB 2065653; US 4447608; US 4564616

合成路线图解说明: The alkylation of diethyl N-(4-aminobenzoyl)glutamate (I) with propargyl bromide (II) in hot ethanol gives diethyl N-[4-(propargylamino)benzoyl]glutamate (III), which is condensed with 2-amino-6-bromomethyl-4-hydroxyquinazoline (IV) by means of triethylamine in hot 2-ethoxyethanol (or CaCO3 in dimethylacetamide) yielding diethyl N-[4-[N-[(2-amino-4-hydroxy-6-quinazolinyl)methyl]prop-2-ynylamino]benzoyl]-L-glutamate (V). Finally, this compound is saponified with NaOH in ethanol-water.