ANTICANCER AGENTS .15. SQUARIC ACID DIETHYL ESTER - A NEW COUPLING REAGENT FOR THE FORMATION OF DRUG BIOPOLYMER CONJUGATES - SYNTHESIS OF SQUARIC ACID ESTER AMIDES AND DIAMIDES

被引：189

作者：

TIETZE, LF ^{[1
]}

ARLT, M ^{[1
]}

BELLER, M ^{[1
]}

GLUSENKAMP, KH ^{[1
]}

JAHDE, E ^{[1
]}

RAJEWSKY, MF ^{[1
]}

机构：

[1] UNIV ESSEN GESAMTHSCH,INST ZELLBIOL TUMORFORSCH,W-4300 ESSEN 1,GERMANY

来源：

CHEMISCHE BERICHTE | 1991年 / 124卷 / 05期

关键词：

SQUARIC ACID; ESTER AMIDES OF; DIAMIDES OF; COUPLING REAGENTS; BIOPOLYMERS; ANTICANCER AGENTS; CONJUGATES;

D O I：

10.1002/cber.19911240539

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

Reaction of squaric acid diethyl ester (1) with a slight excess of a primary or secondary amine 2 in ethanol, dichloromethane or aqueous buffer (pH 7) at 20-degrees-C for 0.3-12 h gives the squaric acid amide esters 3 in mostly excellent yields. Treatment of 3 with amines 2 or 4 in organic solvents in the presence of triethylamine or in aqueous buffer (pH 9) leads to the corresponding symmetrical and unsymmetrical squaric acid diamides 5, respectively. The reaction can be followed by UV spectroscopy.

引用

页码：1215 / 1221

页数：7

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