THE SYNTHESIS OF THE CARBONYL-C-14 ANALOG OF ZATOSETRON MALEATE, A POTENT, LONG-ACTING, ORALLY EFFECTIVE 5-HT3 RECEPTOR ANTAGONIST

被引：2

作者：

OBANNON, DD ^{[1
]}

WHEELER, WJ ^{[1
]}

机构：

[1] ELI LILLY & CO,LILLY RES LAB,LILLY CORP CTR,INDIANAPOLIS,IN 46285

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1991年 / 29卷 / 06期

关键词：

ZATOSETRON MALEATE; 5-HT3 RECEPTOR ANTAGONIST; C-14; LABELED;

D O I：

10.1002/jlcr.2580290603

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Endo-5-chloro-2,3-dihydro-2,2-dimethyl-N-(8-methyl-8-azabicyclo-[3.2.1.]-oct-3-yl-7-benzofurancarboxamide-[carbonyl-C-14] (Z)-2-butenedioate (zatosetron-[C-14] maleate,1), has been prepared from 5-chloro-7-bromo-2,3-dihydro-2,2-dimethylbenzofuran (5) in four radiochemical steps with the reaction of 5 with K14CN/CuCN as the key step. The synthesis of 5 from 2-bromo-4-chlorophenol is also outlined.

引用

页码：625 / 631

页数：7

共 23 条

[21] SYNTHESIS OF [CARBONYL-C-14)-LABELED AND (METHOXY-D3)-LABELED N-[(2RS,3RS)-1-BENZYL-2-METHYL-3-PYRROLIDINYL]-5-CHLORO-2-METHOXY-4-(METHYLAMINO)BENZAMIDE (YM-09151-2) - A NEW POTENT NEUROLEPTIC AGENT
TAMAZAWA, K
ARIMA, H
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1984, 21 (05): : 441 - 453
[22] Bronchodilator Activity of (3R)-3-[[[(3-fluorophenyl)[(3,4,5-trifluorophenyl)methyl]amino] carbonyl]oxy]-1-[2-oxo-2-(2-thienyl)ethyl]-1-azoniabicyclo[2.2.2]octane bromide (CHF5407), a Potent, Long-Acting, and Selective Muscarinic M3 Receptor Antagonist
Villetti, G.
Pastore, F.
Bergamaschi, M.
Bassani, F.
Bolzoni, P. T.
Battipaglia, L.
Amari, G.
Rizzi, A.
Delcanale, M.
Volta, R.
Cenacchi, V.
Cacciani, F.
Zaniboni, M.
Berti, F.
Rossoni, G.
Harrison, S.
Petrillo, P.
Santoro, E.
Scudellaro, R.
Mannini, F.
Geppetti, P. A.
Razzetti, R.
Patacchini, R.
Civelli, M.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS, 2010, 335 (03): : 622 - 635
[23] SYNTHESIS OF [C-14] KT3-671, 2-PROPYL-8-OXO-1-[(2'-(1H-[C-14]TETRAZOLE-5-YL) BIPHENYL-4-YL)METHYL]-4,5,6,7-TETRAHYDRO-CYCLOHEPTIMIDAZOLE, A NOVEL POTENT NONPEPTIDE ANGIOTENSIN-II RECEPTOR ANTAGONIST
UEYAMA, N
YANAGISAWA, T
TOMIYAMA, T
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1995, 36 (10): : 915 - 919

← 1 2 3 →