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5,10-二氮杂-5,6,7,8-四氢叶酸（DDATHF）的一种简化高效合成方法。

A simplified and efficient synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF).

作者信息

Taylor E C, Chaudhari R, Lee K

机构信息

Department of Chemistry, Princeton University, NJ 08544, USA.

出版信息

Invest New Drugs. 1996;14(3):281-5. doi: 10.1007/BF00194531.

DOI:10.1007/BF00194531
PMID:8958183
Abstract

A new and extremely efficient synthesis of DDATHF from 4-vinylbenzoic acid and bromomalondialdehyde as precursors has been developed which proceeds in 48% overall yield.

摘要

已经开发出一种以4-乙烯基苯甲酸和溴代丙二醛为前体的新型高效合成DDATHF的方法，其总产率为48%。

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A simplified and efficient synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF).5,10-二氮杂-5,6,7,8-四氢叶酸（DDATHF）的一种简化高效合成方法。
Invest New Drugs. 1996;14(3):281-5. doi: 10.1007/BF00194531.
2
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本文引用的文献

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Design and synthesis of inhibitors of folate-dependent enzymes as antitumor agents.作为抗肿瘤药物的叶酸依赖性酶抑制剂的设计与合成。
Adv Exp Med Biol. 1993;338:387-408. doi: 10.1007/978-1-4615-2960-6_80.
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Multifactorial resistance to 5,10-dideazatetrahydrofolic acid in cell lines derived from human lymphoblastic leukemia CCRF-CEM.源自人淋巴细胞白血病CCRF-CEM的细胞系对5,10-二去氮四氢叶酸的多因素抗性
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Substrate specificity of mammalian folylpolyglutamate synthetase for 5,10-dideazatetrahydrofolate analogs.
哺乳动物叶酸多聚谷氨酸合成酶对5,10-二去氮四氢叶酸类似物的底物特异性。
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Carrier- and receptor-mediated transport of folate antagonists targeting folate-dependent enzymes: correlates of molecular-structure and biological activity.靶向叶酸依赖性酶的叶酸拮抗剂的载体和受体介导转运：分子结构与生物活性的相关性
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Synthesis of the antileukemic agents 5,10-dideazaaminopterin and 5,10-dideaza-5,6,7,8-tetrahydroaminopterin.
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Synthesis and antifolate activity of 5-methyl-5,10-dideaza analogues of aminopterin and folic acid and an alternative synthesis of 5,10-dideazatetrahydrofolic acid, a potent inhibitor of glycinamide ribonucleotide formyltransferase.氨基蝶呤和叶酸的5-甲基-5,10-二去氮类似物的合成及抗叶酸活性，以及5,10-二去氮四氢叶酸的另一种合成方法，5,10-二去氮四氢叶酸是甘氨酰胺核糖核苷酸甲酰基转移酶的有效抑制剂。
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Synthesis and biological properties of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid.
Arch Biochem Biophys. 1988 Aug 15;265(1):43-9. doi: 10.1016/0003-9861(88)90369-4.
8
A new folate antimetabolite, 5,10-dideaza-5,6,7,8-tetrahydrofolate is a potent inhibitor of de novo purine synthesis.一种新的叶酸抗代谢物，5,10-二去氮-5,6,7,8-四氢叶酸是从头嘌呤合成的有效抑制剂。
J Biol Chem. 1989 Jan 5;264(1):328-33.
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The 6S- and 6R-diastereomers of 5, 10-dideaza-5, 6, 7, 8-tetrahydrofolate are equiactive inhibitors of de novo purine synthesis.
J Biol Chem. 1989 Dec 15;264(35):21047-51.
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Structural features of 5,10-dideaza-5,6,7,8-tetrahydrofolate that determine inhibition of mammalian glycinamide ribonucleotide formyltransferase.决定对哺乳动物甘氨酰胺核糖核苷酸甲酰基转移酶抑制作用的5,10-二脱氮-5,6,7,8-四氢叶酸的结构特征。
Biochemistry. 1991 Feb 19;30(7):1997-2006. doi: 10.1021/bi00221a037.