Synthesis of metabolites of dapagliflozin: an SGLT2 inhibitor

被引：0

作者：

Karumanchi, Kishore ^{[1
,2
]}

Natarajan, Senthil Kumar ^{[1
]}

Chavakula, Ramadas ^{[1
]}

Korupolu, Raghu Babu ^{[2
]}

Bonige, Kishore Babu ^{[2
]}

Peruri, Badarinadh Gupta ^{[3
]}

机构：

[1] Chemical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd., Survey No. 71 & 72, Indrakaran Village, Kandi Mandal, Sangareddy District,Telangana State,502329, India

[2] Department of Engineering Chemistry, A. U. College of Engineering (A), Andhra University, Visakhapatnam,Andhra Pradesh,530003, India

[3] Analytical Research and Development, APL Research Centre-II, Aurobindo Pharma Ltd, Survey No. 71 & 72, Indrakaran Village, Kandi Mandal, Sangareddy District,Telangana State,502329, India

来源：

Journal of Chemical Sciences | 2020年 / 132卷 / 01期

关键词：

Biomolecules;

D O I：

暂无

中图分类号：

学科分类号：

摘要：

Abstract: Dapagliflozin is one of the gliflozin class drugs, useful for the treatment of type-2 diabetes. Dapagliflozin undergoes extensive metabolism and transforms to metabolites in humans. The contribution of pharmacologically active metabolites in drug discovery and development is significant. A streamlined synthetic approach is devised to access three metabolites of dapagliflozin namely, benzylic hydroxy dapagliflozin, oxo dapagliflozin and desethyl dapagliflozin. Two synthetic protocols have been proposed for the synthesis of benzylic hydroxy dapagliflozin and oxo dapagliflozin. An enantioselective deethylation of dapagliflozin is also reported. Graphic abstract: Synthesis of three metabolites of Dapagliflozin namely benzylic hydroxy dapagliflozin, oxo dapagliflozin and desethyl dapagliflozin is reported from commercially accessible raw materials.[Figure not available: see fulltext.] © 2020, Indian Academy of Sciences.

引用

共 50 条

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Karumanchi, Kishore
Natarajan, Senthil Kumar
Chavakula, Ramadas
Korupolu, Raghu Babu
Bonige, Kishore Babu
Peruri, Badarinadh Gupta
[J]. JOURNAL OF CHEMICAL SCIENCES, 2020, 132 (01)
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KISHORE KARUMANCHI
SENTHIL KUMAR NATARAJAN
RAMADAS CHAVAKULA
RAGHU BABU KORUPOLU
KISHORE BABU BONIGE
BADARINADH GUPTA PERURI
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