THE SYNTHESIS OF [H-3] LOSARTAN, [H-3] L-158,641 AND [H-3] L-158,809

被引：5

作者：

RIVERO, RA ^{[1
]}

CHAKRAVARTY, PK ^{[1
]}

CHEN, R ^{[1
]}

GREENLEE, WJ ^{[1
]}

ROSEGAY, A ^{[1
]}

SIMPSON, R ^{[1
]}

机构：

[1] MERCK RES LABS,DEPT ANIM & EXPLORATORY DRUG METAB,RAHWAY,NJ 07065

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 04期

关键词：

D O I：

10.1016/S0960-894X(01)81228-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Selective radioligands of the angiotensin II AT1 receptor subtype have been prepared. Radiolabeled Losartan (DuP 753)1,2, L-158,641 (EXP3174)3 and L-158,8094,5 were prepared from a common bromobiphenyl intermediate. The key step in the synthesis is the selective aromatic monobromination of 2-cyano-4'-methylbiphenyl.

引用

页码：557 / 560

页数：4

共 17 条

[1]

BOVY PR, 1992, RECENT ADV NONPEPTID, V2, pB17

[2] NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS - THE DISCOVERY OF A SERIES OF N-(BIPHENYLYLMETHYL)IMIDAZOLES AS POTENT, ORALLY ACTIVE ANTIHYPERTENSIVES [J].

CARINI, DJ ;

DUNCIA, JV ;

ALDRICH, PE ;

CHIU, AT ;

JOHNSON, AL ;

PIERCE, ME ;

PRICE, WA ;

SANTELLA, JB ;

WELLS, GJ ;

WEXLER, RR ;

WONG, PC ;

YOO, SE ;

TIMMERMANS, PBMWM .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (08) :2525-2547

[3]

CHEN TB, 1992, UNPUB CHARACTERIZATI

[4] [H-3] DUP-753, A HIGHLY POTENT AND SPECIFIC RADIOLIGAND FOR THE ANGIOTENSIN-II-1 RECEPTOR SUBTYPE [J].

CHIU, AT ;

MCCALL, DE ;

ALDRICH, PE ;

TIMMERMANS, PBMWM .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1990, 172 (03) :1195-1202

[5] DUP-532 - A 2ND GENERATION OF NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONISTS [J].

CHIU, AT ;

CARINI, DJ ;

DUNCIA, JV ;

LEUNG, KH ;

MCCALL, DE ;

PRICE, WA ;

WONG, PC ;

SMITH, RD ;

WEXLER, RR ;

TIMMERMANS, PBMWM ;

CHANG, RSL ;

LOTTI, VJ .

BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1991, 177 (01) :209-217

[6] CATALYTIC DEHALOGENATION WITH SODIUM BOROHYDRIDE [J].

EGLI, RA .

HELVETICA CHIMICA ACTA, 1968, 51 (08) :2090-&

[7]

EVANS EA, 1974, TRITIUM ITS COMPOUND, P190

[8] RENIN INHIBITORS [J].

GREENLEE, WJ .

MEDICINAL RESEARCH REVIEWS, 1990, 10 (02) :173-236

[9]

Janssen D. E., 1963, ORG SYNTH, VIV, P547

[10] POTENT, ORALLY ACTIVE IMIDAZO[4,5-B]PYRIDINE-BASED ANGIOTENSIN-II RECEPTOR ANTAGONISTS [J].

MANTLO, NB ;

CHAKRAVARTY, PK ;

ONDEYKA, DL ;

SIEGL, PKS ;

CHANG, RS ;

LOTTI, VJ ;

FAUST, KA ;

CHEN, TB ;

SCHORN, TW ;

SWEET, CS ;

EMMERT, SE ;

PATCHETT, AA ;

GREENLEE, WJ .

JOURNAL OF MEDICINAL CHEMISTRY, 1991, 34 (09) :2919-2922

← 1 2 →