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Vol. 24 No. 8 (2012): Vol 24 Issue 8

Lewis Acid Mediated Nucleophilic Ring-Opening of 1-Benzhydryl Azetidine-3-ol with Aryl Alcohols: A Formal Synthesis of Carvedilol

V.V.R.M. Krishna Reddy
Research & Development, Inogent Laboratories Private Limited, (A GVK BIO Company), 28A, IDA, Nacharam, Hyderabad-500 076, India ; Centre for Pharmaceutical Sciences, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad-500 072, India
H. Ramamohan
Aptuit Laurus Private Limited, ICICI Knowledge Park, Turkapally, Shameerpet, Hyderabad500 078, India
A. Ganesh
Research & Development, Inogent Laboratories Private Limited, (A GVK BIO Company), 28A, IDA, Nacharam, Hyderabad-500 076, India
K. Srinivas
Research & Development, Inogent Laboratories Private Limited, (A GVK BIO Company), 28A, IDA, Nacharam, Hyderabad-500 076, India
K. Mukkanti
Centre for Pharmaceutical Sciences, Jawaharlal Nehru Technological University, Kukatpally, Hyderabad-500 072, India
G. Madhusudhan
Research & Development, Inogent Laboratories Private Limited, (A GVK BIO Company), 28A, IDA, Nacharam, Hyderabad-500 076, India

Corresponding Author(s) : G. Madhusudhan

madhusudhan.gutta@inogent.com; madhusudhan.gutta@yahoo.com

Asian Journal of Chemistry, Vol. 24 No. 8 (2012): Vol 24 Issue 8

Abstract

Lewis acid mediated nucleophilic azetidine ring opening of 1-benzhydrylazetidine-3-ol with phenolic oxygen as nucleophile is reported. This approach was also utilized successfully to synthesize, carvedilol a b-adrenergic blocking agent.

Keywords

1-Benzhydrylazetidin-3-ol Lewis acid Substituted phenols Azetidine ring opening Carvedilol β-Adrenergic blocking agent
Krishna Reddy, V., Ramamohan, H., Ganesh, A., Srinivas, K., Mukkanti, K., & Madhusudhan, G. (2012). Lewis Acid Mediated Nucleophilic Ring-Opening of 1-Benzhydryl Azetidine-3-ol with Aryl Alcohols: A Formal Synthesis of Carvedilol. Asian Journal of Chemistry, 24(8), 3468–3472. Retrieved from https://asianpubs.org/index.php/ajchem/article/view/9397
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