Tsunoda, Takashi’s team published research in Organic Process Research & Development in 2005-10-31 | 112-63-0

Organic Process Research & Development published new progress about Acid hydrolysis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, HPLC of Formula: 112-63-0.

Tsunoda, Takashi; Yamazaki, Atsuki; Mase, Toshiyasu; Sakamoto, Shuichi published the artcile< A Scalable Process for the Synthesis of 2-Methyl-1,4,5,6-tetrahydroimidazo[4,5-d][1]benzazepine Monohydrate and 4-[(Biphenyl-2-ylcarbonyl)amino]benzoic Acid: Two New Key Intermediates for the Synthesis of the AVP Antagonist Conivaptan Hydrochloride>, HPLC of Formula: 112-63-0, the main research area is safety methyltetrahydroimidazo benzazepine intermediate preparation scale up green chem; biphenylylcarbonyl aminobenzoic acid intermediate preparation vasopressin receptor antagonist.

A process for the multikilogram synthesis of the dual vasopressin-receptor antagonist, conivaptan hydrochloride, was developed. This method relies on the introduction of operationally simple chem. during the final stages of the process when two key intermediates, isolated by crystallization, are reacted to assemble the final mol. A three-stage sequence was developed for the synthesis of the first key amine hydrate intermediate, and modifications of the original process are described. Major strategic improvements were achieved in defining the final route to the side chain precursor mol., which is the second key intermediate. These advances revolve around the acylation of an unprotected amino benzoic acid and subsequent high-yield telescoped processes for the synthesis of 4-[(biphenyl-2-ylcarbonyl)amino]benzoic acid. This method leads to a 4-fold increase in the overall yield of the target materials, circumvents the restricted synthetic intermediates, and constitutes a safe, reliable, adaptable, environmentally friendly, and cost-effective approach with improved manipulability.

Organic Process Research & Development published new progress about Acid hydrolysis. 112-63-0 belongs to class esters-buliding-blocks, and the molecular formula is C19H34O2, HPLC of Formula: 112-63-0.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics