863762-20-3

Upstream product

• 863762-10-1 2,2-dimethylpropionic acid 7-chloro-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl ester 
• 30459-70-2 2-methyl-4-nitrobenzoyl chloride 
• 863762-02-1 2,2-dimethylpropionic acid 4-[(E)-hydroxyimino]-7-chloro-1,2,3,4-tetrahydronaphthalen-1-yl ester 
• 804498-94-0 (rac)-7-chloro-4-oxo-1,2,3,4-tetrahydronaphthalen-1-yl pivalate 

Downstream Products

• 150683-30-0 tolvaptan 
• 863762-24-7 2,2-dimethylpropionic acid 7-chloro-1-(4-amino-2-methylbenzoyl)-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl ester 

Relevant academic research and scientific papers

Method of preparing benzazepines and derivatives thereof

The invention relates to a method of preparing benzazepine compounds having general formula (IA) consisting in reacting at least one compound having general formula (IIA) with an olefin, the compound thus obtained then being cyclised such as to produce tetralone, followed by the oxime derivative of same, which, by transformation by a Beckmann rearrangement, gives rise to the desired compounds.

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

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.