[EN] PROCESS FOR THE SYNTHESIS OF CYCLIC CARBAMATES<br/>[FR] PROCÉDÉ DE SYNTHÈSE DE CARBAMATES CYCLIQUES
申请人:LONZA AG
公开号:WO2012048886A1
公开(公告)日:2012-04-19
The invention is directed to a process for the preparation of a cyclic carbamate starting with o-aminobenzyl alcohol and/or a suitable salt thereof, which is reacted with a cyclisation agent selected from phosgene, diphosgene, triphosgene and mixtures thereof, and in that the reaction carried out in the presence of an aqueous base, and a water-immiscible organic solvent, said organic solvent mainly comprising at least one compound selected from C2-5-alkyl C2-5-carboxylates and mixtures of at least one C2-5-alkyl C2-5-carboxylate with at least one C5-8-alkane.
作者:Alan R. Katritzky、Qiu-He Long、Ping Lue、Andrzej Jozwiak
DOI:10.1016/s0040-4020(01)81471-x
日期:——
A new, facile preparation of enamines was achieved via a two-step sequence: (i) the ready formation of an N-(α-aminoalkyl)benzotriazole derivative from equimolar amounts of benzotriazole, an aldehyde, and a secondary amine, (ii) the elimination of benzotriazole from the derivative by sodium hydride in tetrahydrofuran (THF). The method provides enamines in good overall yields based on the quantity of
A compound of formula [I-W]:
wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
翻译结果为:具有公式[I-W]的化合物:其中每个符号如描述中定义,或其药物可接受的盐。
NOVEL TRIAZOLE COMPOUNDS I
申请人:Hernandez Maria-Clemencia
公开号:US20120115844A1
公开(公告)日:2012-05-10
The present invention is concerned with novel triazole compounds of formula (I)
wherein A, X, Y, Z, R
1
, R
2
, and R
3
are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
本发明涉及具有以下式(I)的新型三唑化合物,
其中A、X、Y、Z、R1、R2和R3如本文所述,以及其药学上可接受的盐和酯。本发明的活性化合物具有对GABA A α5受体的亲和力和选择性。此外,本发明涉及制备具有式(I)的化合物,包括它们的药物组合物以及它们作为药物的用途。
[EN] TRIAZOLE DERIVATIVES AND THEIR USE FOR NEUROLOGICAL DISORDERS<br/>[FR] DÉRIVÉS DE TRIAZOLE ET LEUR UTILISATION POUR DES TROUBLES NEUROLOGIQUES
申请人:HOFFMANN LA ROCHE
公开号:WO2012062687A1
公开(公告)日:2012-05-18
The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, Z, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of present invention have affinity and selectivity for the GABA A α5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
本发明涉及一种新型三唑化合物,其化学式为(I),其中A、X、Y、Z、R1、R2和R3如本文所述,以及其药学上可接受的盐和酯。本发明的活性化合物具有对GABA A α5受体的亲和力和选择性。此外,本发明涉及制备化合物(I)的方法,包括它们的药物组合物以及它们作为药物的用途。