PREPARATION OF 1,2-DIMETHOXY-4-(BIS-DIETHYLAMINOETHYL-[C-14]-AMINO)-5-BROMOBENZENE

被引：0

作者：

WANG, TST ^{[1
]}

FAWWAZ, RA ^{[1
]}

VANHEERTUM, RH ^{[1
]}

机构：

[1] COLUMBIA UNIV COLL PHYS & SURG,DEPT RADIOL,DIV NUCL MED,NEW YORK,NY 10032

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1993年 / 33卷 / 11期

关键词：

ANTIMALARIAL AGENT; RC-12-[C-14; CHLORINATION; GRIGNARD REAGENT; BIS-N-ALKYLATION;

D O I：

10.1002/jlcr.2580331103

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

1,2-Dimethoxy-4-(bis-diethylaminoethyl-[C-14] -amino)-5-bromobenzene (III) was synthesized for in vivo pharmacokinetic and pharmacodynamic evaluation. The synthesis of (III) was easily obtained by the direct alkylation of 1,2-dimethoxy-5-bromo-aniline with beta-diethylaminoethyl chloride-ethylene-[C-14], using CH3MgCl as the proton abstractor. Compound III was obtained with a 22.3% yield. The specific activity was 2.2mCi/mmol, with a radiochemical purity of >99%.

引用

页码：1007 / 1012

页数：6

共 50 条

[21] 1,2-DITHIA-CYCLOPENTENES .14. DIAMINO-DIALKOXYCARBONYL-C4-COMPOUNDS FROM 4-CHLORO-5-AMINO-1,2-DITHIA-CYCLOPENTEN-3-ONES
BOBERG, F
NIEMANN, H
KIRCHHOF.K
ANNALEN DER CHEMIE-JUSTUS LIEBIG, 1969, 728 (NOV): : 32 - &
[22] METABOLISM AND TISSUE DISTRIBUTION OF (1,4,5,8-C-14)-1,2-DICHLORONAPHTHALENE IN RATS
CHU, I
SECOURS, V
VILLENEUVE, DC
VIAU, A
BULLETIN OF ENVIRONMENTAL CONTAMINATION AND TOXICOLOGY, 1977, 18 (02) : 177 - 183
[23] Effective synthesis of 4,5-dibromobenzo[1,2-c:3,4-c']-bis([1,2,5]thiadiazole) by bromination of benzo[1,2-c:3,4-c']-bis([1,2,5]thiadiazole)
Chechulina, Alexandra S.
Konstantinova, Lidia S.
Obruchnikova, Natalia V.
Knyazeva, Ekaterina A.
Kan, Bin
Duan, Tainan
Chen, Yongsheng
Aysin, Rinat A.
Rakitin, Oleg A.
CHEMISTRY OF HETEROCYCLIC COMPOUNDS, 2024, 60 (7-8) : 403 - 408
[24] A BIODISTRIBUTION STUDY OF 1-C-14-1,2-CYCLOHEXANEDIONE-BIS(4-DIETHYLENOXYTHIOSEMICARBAZONE), A POTENTIAL ANTITUMOUR AGENT
VARUGHESE, A
WILLIAMS, L
MORGAN, HK
DRUGS UNDER EXPERIMENTAL AND CLINICAL RESEARCH, 1984, 10 (02) : 67 - 74
[25] PREPARATION OF 5-AMINO-1,2-DIHYDRO-4-(1-METHYL-4-PIPERIDINYL)PYRROL-3-ONES
Chalyk, Bohdan A.
Tverdokhlebov, Anton V.
Iminov, Rustam T.
Tolmachev, Andrey A.
HETEROCYCLES, 2009, 78 (08) : 2021 - 2032
[26] SYNTHESIS OF 1-[4-[3-(N-METHYL-N-[3,4-DIMETHOXY-BETA-PHENETHYL]AMINO][3-C-14]PROPYLOXY]BENZENESULFONYL]-2-ISOPROPYL-INDOLIZINE OR [C-14] SR-33557
DEMOTTE, R
DEBLATON, M
WINAND, M
CALLAERT, M
SION, R
GUBIN, J
CHATELAIN, P
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1990, 28 (10): : 1135 - 1141
[27] SYNTHESIS AND C-14 LABELING OF N,N-DI-2-CHLOROETHYL-4-AMINO-2-METHYL-1-METHOXYNAPHTHALENE OR MITOCLOMINE
MADELMONT, JC
MOREAU, MF
GODENECHE, D
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1978, 14 (02): : 281 - 291
[28] DERIVATIVES OF 1,3-BENZODIOXOLES .47. PREPARATION AND REACTIONS OF 4,8-DIMETHOXY-BIS[1,3]DIOXOLO[4,5]BENZO-[1,2-D-1,'2'-F][1,3]DIOXEPINE
DALLACKER, F
COERVER, W
ZEITSCHRIFT FUR NATURFORSCHUNG SECTION B-A JOURNAL OF CHEMICAL SCIENCES, 1983, 38 (03): : 383 - 391
[29] POTENTIAL-DRUGS LABELED WITH C-14 .2. SYNTHESIS OF 1-CYANO-3-IMINO-8,9-DIMETHOXY-3,4,5,6-TETRAHYDRO-THIAZOLO[4,3-A]ISOQUINOLINE HYDROCHLORIDE
KOLTAI, E
ZOLYOMI, G
KOMAROMY, P
BANFI, D
SZUTS, T
TAKACS, K
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1981, 18 (08): : 1107 - 1113
[30] Crystal structure of trans-1,2-bis(pyridinium-4-yl) ethylene bis(2-carboxy-4-bromobenzoate) - water (1/4), C14H14BrNO6
Yuan, Wei-Wei
ZEITSCHRIFT FUR KRISTALLOGRAPHIE-NEW CRYSTAL STRUCTURES, 2022, 237 (02): : 289 - 291

← 1 2 3 4 5 →