An efficient, scalable synthesis of the HIV reverse transcriptase inhibitor Ziagen® (1592U89)

被引：74

作者：

Daluge, SM ^{[1
]}

Martin, MT

Sickles, BR

Livingston, DA

机构：

[1] Glaxo Wellcome Inc, Div Med Chem, Res Triangle Pk, NC 27709 USA

[2] Glaxo Wellcome Inc, Chem Dev Div, Res Triangle Pk, NC 27709 USA

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 2000年 / 19卷 / 1-2期

关键词：

D O I：

10.1080/15257770008033011

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Ziagen(R), (IS, cis)-4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol, was synthesized from (IS,4R)-azabicyclo[2.2.1]hept-5-en-3-one by efficient processes which bypass problematic steps in earlier routes. 2-Amino-4,6-dichloro-5-formamidopyrimidine is a key intermediate which makes possible an efficient construction of the purine from a chiral cyclopentenyl precursor.

引用

页码：297 / 327

页数：31

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