A flexible approach for the preparation of substituted benzazepines: Application to the synthesis of tolvaptan

Alejandro Cordero-Vargas; Béatrice Quiclet-Sire; Samir Z. Zard

doi:10.1016/j.bmc.2006.05.070

A flexible approach for the preparation of substituted benzazepines: Application to the synthesis of tolvaptan

Alejandro Cordero-Vargas
, Béatrice Quiclet-Sire
, Samir Z. Zard

Laboratoire de Synthèse Organique

Research output: Contribution to journal › Article › peer-review

Abstract

A practical preparation of benzazepine derivatives using a series of radical and ionic reactions is reported. This approach was applied to the synthesis of tolvaptan, a very promising vasopressin V₂ receptor antagonist currently in clinical trials.

Original language	English
Pages (from-to)	6165-6173
Number of pages	9
Journal	Bioorganic and Medicinal Chemistry
Volume	14
Issue number	18
DOIs	https://doi.org/10.1016/j.bmc.2006.05.070
Publication status	Published - 15 Sept 2006
Externally published	Yes

Keywords

Beckmann rearrangement
Benzazepines
Tolvaptan
Xanthate

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10.1016/j.bmc.2006.05.070

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title = "A flexible approach for the preparation of substituted benzazepines: Application to the synthesis of tolvaptan",

abstract = "A practical preparation of benzazepine derivatives using a series of radical and ionic reactions is reported. This approach was applied to the synthesis of tolvaptan, a very promising vasopressin V2 receptor antagonist currently in clinical trials.",

keywords = "Beckmann rearrangement, Benzazepines, Tolvaptan, Xanthate",

author = "Alejandro Cordero-Vargas and B{\'e}atrice Quiclet-Sire and Zard, \{Samir Z.\}",

year = "2006",

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day = "15",

doi = "10.1016/j.bmc.2006.05.070",

language = "English",

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journal = "Bioorganic and Medicinal Chemistry",

issn = "0968-0896",

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T1 - A flexible approach for the preparation of substituted benzazepines

T2 - Application to the synthesis of tolvaptan

AU - Cordero-Vargas, Alejandro

AU - Quiclet-Sire, Béatrice

AU - Zard, Samir Z.

PY - 2006/9/15

Y1 - 2006/9/15

N2 - A practical preparation of benzazepine derivatives using a series of radical and ionic reactions is reported. This approach was applied to the synthesis of tolvaptan, a very promising vasopressin V2 receptor antagonist currently in clinical trials.

AB - A practical preparation of benzazepine derivatives using a series of radical and ionic reactions is reported. This approach was applied to the synthesis of tolvaptan, a very promising vasopressin V2 receptor antagonist currently in clinical trials.

KW - Beckmann rearrangement

KW - Benzazepines

KW - Tolvaptan

KW - Xanthate

U2 - 10.1016/j.bmc.2006.05.070

DO - 10.1016/j.bmc.2006.05.070

M3 - Article

C2 - 16782344

AN - SCOPUS:33747104133

SN - 0968-0896

VL - 14

SP - 6165

EP - 6173

JO - Bioorganic and Medicinal Chemistry

JF - Bioorganic and Medicinal Chemistry

IS - 18

ER -

A flexible approach for the preparation of substituted benzazepines: Application to the synthesis of tolvaptan

Abstract

Keywords

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