1-Alkyl-2,4-dihydro-1H-pyrazino[2,1-b]quinazoline-3,6-diones as glycine templates.: Synthesis of Fiscalin B

被引：24

作者：

Hernández, F ^{[1
]}

Buenadicha, FL ^{[1
]}

Avendaño, C ^{[1
]}

Söllhuber, M ^{[1
]}

机构：

[1] Univ Complutense, Fac Farm, Dept Quim Organ & Farmaceut, E-28040 Madrid, Spain

来源：

TETRAHEDRON-ASYMMETRY | 2002年 / 12卷 / 24期

关键词：

D O I：

10.1016/S0957-4166(02)00027-7

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

An excess of base allows the regio- and diastereoselective alkylation at C(4) of the glycine templates 1-methyl(isopropyl)-2,4-dihydro-1H-pyrazino[2,1-b]quinazoline-3,6-diones 9a and 9b without the need for N(2)-protecting groups. While the alkylation of 9a gave exclusively the 1,4-anti-isomers, the isopropyl derivative 9b required much longer reaction times and occurred with lower diastereoselectivity. Fiscalin B 3 was obtained by alkylation of 9b with N-Boc-3-indolylmethyl bromide followed by indole deprotection. (C) 2002 Elsevier Science Ltd. All rights reserved.

引用

页码：3387 / 3398

页数：12

共 36 条

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