Synthesis of tritiated N-[4-(2,4-diaminopteridine-6-methyl)-3,4-dihydro-2H-1,4-benzothiazine-7-carbonyl]-L-homo glutamic acid (MX-68)

被引：0

作者：

Matsuoka, H

Kuroki, T

Yano, K

Takeda, Y

机构：

[1] Fuji Gotemba Research Laboratories, Chugai Pharmaceutical Co., Ltd., Gotemba, Shizuoka 412

来源：

JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS | 1997年 / 39卷 / 05期

关键词：

N-[4-(2,4-diaminopteridine-6-methyl)-3,4-dihydro-2H-1,4-benzothiazine-7-carbonyl]-7-homoglutamic acid; MX-68; methotrexate; 9-H-3(1)]MX-68; sodium borotritiide;

D O I：

10.1002/(SICI)1099-1344(199705)39:5<363::AID-JLCR982>3.0.CO;2-O

中图分类号：

Q5 [生物化学];

学科分类号：

071010 ; 081704 ;

摘要：

Synthesis of tritiated N-[4-(2,4-diaminopteridine-6-methyl)-3,4-dihydro-2H-1,4-benzothiazine-7-carbonyl]-L-homoglutamic acid, [9-H-3(1)]MX-68 (3), is described. [9-H-3(1)]MX-68 (3) was prepared via tritiation at the carbonyl group in 2,4-bis(butanoylamino)-6-formylpteridine (7) with sodium borotritiide.

引用

页码：363 / 368

页数：6

共 50 条

[1] Synthesis of tritiated N-[4-(2,4-diaminopteridine-6-methyl)-3,4-dihydro-2H-1,4- benzothiazine-7-carbonyl]-L-homo glutamic acid (MX-68)
Matsuoka, Hiroharu
Kuroki, Toshio
Yano, Keiichi
Takeda, Yasuhisa
Journal of Labelled Compounds and Radiopharmaceuticals, 1997, 39 (05): : 363 - 368
[2] Synthesis of Tritiated N-[4-(2,4-Diaminopteridine-6-Methyl)- 3,4- Dihydro-2H-1,4-Benzothiazine-7-Carbonyl]$ MIN@L- Homo Glutamic Acid (MX-68)
Matsuoka, H.
Kuroki, T.
Yano, K.
Takeda, Y.
Journal of Labelled Compounds and Radiopharmaceuticals, 39 (05):
[3] Carrier-mediated hepatobiliary transport of a novel antifolate, N-[4-[(2,4-diamminopteridine-6-yl) methyl]-3,4-dihydro-2H-1,4-benzothiazin-7-yl]carbonyl-L- homoglutamic acid, in rats
Han, YH
Kato, Y
Watanabe, Y
Terao, K
Asoh, Y
Sugiyama, Y
DRUG METABOLISM AND DISPOSITION, 2001, 29 (04) : 394 - 400
[4] Synthesis and biological activity of Na-[4-[N-[(3,4-dihydro-2-methyl-4-oxo-6-quinazolinyl)methyl]-N-propargylamino]phenyl-acetyl]-L-glutamic acid
Kusakiewicz-Dawid, A
Bugaj, M
Dzik, JM
Golos, B
Winska, P
Pawelczak, K
Rzeszotarska, B
Rode, W
ACTA BIOCHIMICA POLONICA, 2002, 49 (01) : 197 - 203
[5] SYNTHESIS OF N-([2-([(2-AMINO-3,4-DIHYDRO-4-OXO-6-PTERIDINYL)METHYL]AMINO)-5-PYRAZINYL]CARBONYL)-L-GLUTAMIC ACID (2',5'-DIAZAFOLIC ACID
NAKAHARA, Y
SEKIKAWA, I
KAKIMOTO, S
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1975, 12 (05) : 1073 - 1074
[6] Synthesis of N-{4-[(2,4-diamino-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid and N-{4-[(2-amino-4-oxo-5-methyl-4,7-dihydro-3H-pyrrolo[2,3-d]pyrimidin-6-yl)thio]benzoyl}-L-glutamic acid as dual inhibitors of dihydrofolate reductase and thymidylate synthase and as potential antitumor agents
Gangjee, A
Lin, X
Kisliuk, RL
McGuire, JJ
JOURNAL OF MEDICINAL CHEMISTRY, 2005, 48 (23) : 7215 - 7222
[7] Conformationally tailored N-[(2-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazin-2-yl)carbonyl]proline templates as molecular tools for the design of peptidomimetics.: Design and synthesis of fibrinogen receptor antagonists
Stefanic, P
Simoncic, Z
Breznik, M
Plavec, J
Anderluh, M
Addicks, E
Athanassios, GC
Kikelj, D
ORGANIC & BIOMOLECULAR CHEMISTRY, 2004, 2 (10) : 1511 - 1517
[8] SYNTHESIS OF N-[4-[2-(2,4-DIAMINO-1,6-DIHYDRO-6-OXO-5-PYRIMIDINYL)-ETHYLAMINO]BENZOYL]-L-GLUTAMIC ACID - AN ACYCLIC ANALOG OF 5,6,7,8-TETRAHYDROFOLIC ACID
KELLEY, JL
MCLEAN, EW
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1990, 27 (02) : 459 - 461
[9] SYNTHESIS OF N-[P-[[(2-AMINO-3,4-DIHYDRO-4-THIOXO-6-PTERIDINYL)METHYL]-METHYLAMINO]BENZOYL]-L-GLUTAMIC ACID (N10-METHYL-4-THIOFOLIC ACID) AND RELATED COMPOUNDS
ELLIOTT, RD
TEMPLE, C
FRYE, JL
MONTGOMERY, JA
JOURNAL OF HETEROCYCLIC CHEMISTRY, 1973, 10 (06) : 1071 - 1072
[10] Synthesis of Substituted 4-(5-Alkyl-thiazol-2-ylmethyl)-3,4-dihydro-2H-1,4-benzoxazines and 5-(2,3-Dihydro-1,4-benzoxazin-4-ylmethyl)-4-methyl-1-phenyl-]-1H-pyrazol-3-ylamine
Mizar, Pushpak
Myrboh, Bekington
JOURNAL OF HETEROCYCLIC CHEMISTRY, 2009, 46 (01) : 39 - 43

← 1 2 3 4 5 →