SYNTHESIS OF NOVEL HMG-COA REDUCTASE INHIBITORS .1. NAPHTHALENE ANALOGS OF MEVINOLIN

被引：0
|
作者：
NOVAK, L
ROHALY, J
POPPE, L
HORNYANSZKY, G
KOLONITS, P
ZELEI, I
FEHER, I
FEKETE, J
SZABO, E
ZAHORSZKY, U
JAVOR, A
SZANTAY, C
机构：
[1] TECH UNIV BUDAPEST, INST ORGAN CHEM, SZT GELLERT TER 4, H-1521 BUDAPEST, HUNGARY
[2] HUNGARIAN ACAD SCI, CENT RES INST CHEM, H-1525 BUDAPEST, HUNGARY
[3] TECH UNIV BUDAPEST, INST GEN & ANALYT CHEM, H-1521 BUDAPEST, HUNGARY
[4] UNIV KARLSRUHE, INST ORGAN CHEM, W-7500 KARLSRUHE 1, GERMANY
[5] GEDEON RICHTER CHEM WORKS LTD, H-1103 BUDAPEST, HUNGARY
来源：
LIEBIGS ANNALEN DER CHEMIE | 1992年 / 02期
关键词：
HMG-COA REDUCTASE INHIBITORS; NAPHTHYLACETATES; PIG LIVER ESTERASE; GLUTARATE; 3-HYDROXY; LACTONES;
D O I：
暂无
中图分类号：
O6 [化学];
学科分类号：
0703 ;
摘要：
The title compounds 2 and their corresponding (6S) epimers 18 are prepared in several steps by starting with chiral formyl ester 5, and alpha-tetralones 10: (1) coupling reaction with the ylide generated from 11 to yield unsaturated ester 13, (2) reduction to the corresponding alcohol 14, (3) addition of the Grignard reagent derived from 14 to formyl ester 5 to afford the hydroxy esters 16 and 17, and (4) lactonization. This procedure is also used to synthesize the beta-naphthyl analogs 29 and 30. Some results obtained from HMG-CoA reductase inhibitor screening are also reported.
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页码：145 / 157
页数：13
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