[5--4--13--2-]---2-[4-2-] N-[5-AMINOSULFONYL-4-METHYL-13-THIAZOL-2-YL]-N-METHYL-2-[4-2-PYDINYLPHENYL]ACETAMIDE MESYLATE MONOHYDRATE

• Main Authors: GRUNENBERG ALFONS, REHSE JOACHIM, VOEGTLI KURT, SCHWAB WILFRIED, KEIL BIRGIT, LENDER ANDREAS, BIRKMANN ALEXANDER, HAAG DIETER
• Format: Patent
• Language: English; Korean
• Published: 06.09.2019
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

본 발명은, 독성 유기 주석 화합물을 방지하면서, 보론산(boronic acid) 유도체 또는 보롤란(borolane) 시약을 사용하는 것에 의한 N-[5-(아미노설포닐)-4-메틸-1,3-티아졸-2-일]-N-메틸-2-[4-(2-피리디닐)페닐]아세트아미드와 그 메실레이트 일수화물 염의 향상되고 단축된 합성에 관한 것이고, 증가된 장기간의 안정성과 약제 조성물로부터의 방출 동역학(release kinetics)을 입증한 N-[5-(아미노설포닐)-4-메틸-1,3-티아졸-2-일]-N-메틸-2-[4-(2-피리디닐)페닐]아세트-아미드의 메실레이트 일수화물 염에 관한 것이다. The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions.