Cyanomethylamines and azidomethylamines: new general methods of the synthesis and transformations
摘要:
Simple and efficient methods have been developed to obtain cyanomethylamines and azidomethylamines using reactions of methoxymethylamines with TMSCN and TMSN3, respectively. In the case of dimethylformamide dimethylacetal, only one MeO group was substituted with CN, and an unexpected direction of the subsequent azidation was found. Adducts of azidomethylamines with DMAD were studied, and the base-catalyzed isomerization of symmetric triazoles into non-symmetric ones was revealed.
DOI:
10.1016/j.mencom.2009.09.018
作为产物:
描述:
甲醇 、 苄胺 在
copper oxide complexed with a nitrogen containing ligand supported on carbon 、 air 作用下,
160.0 ℃
、2.0 MPa
条件下,
反应 0.2h,
以78%的产率得到N-(methoxymethyl)phenylmethylamine
[EN] INDAZOLE- AND PYRROLOPYRIDINE-DERIVATIVE AND PHARMACEUTICAL USE THEREOF<br/>[FR] DÉRIVÉ D'INDAZOLE ET PYRROLOPYRIDINE ET UTILISATION PHARMACEUTIQUE DE CELUI-CI
申请人:DAINIPPON SUMITOMO PHARMA CO
公开号:WO2012169649A1
公开(公告)日:2012-12-13
The present invention relates to a novel indazole- or pyrrolopyridine-derivative, represented by the formula (1) below, that has an agonistic action or a partial agonistic action against serotonin-4 receptor, and a pharmaceutical composition comprising the same. Formula (1) [wherein each substituent is as defined in claim 1]
[EN] CARBAMATE AND UREA INHIBITORS OF 11BETA-HYDROXYSTEROID DEHYDROGENASE 1<br/>[FR] INHIBITEURS DE LA 11BÊTA-HYDROXYSTÉROÏDE-DÉSHYDROGÉNASE 1 À BASE DE CARBAMATES ET D'URÉE
申请人:VITAE PHARMACEUTICALS INC
公开号:WO2010141424A1
公开(公告)日:2010-12-09
This invention relates to novel compounds of the invention pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11β-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.
[EN] THIAZOLE DERIVATIVES AND THEIR USE AS VAP-1 INHIBITORS<br/>[FR] DERIVES DE THIAZOLE ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE VAP-1
申请人:FUJISAWA PHARMACEUTICAL CO
公开号:WO2004067521A1
公开(公告)日:2004-08-12
A compound of the formula (I): R1-NH-X-Y-Z (I) wherein R1 is acyl; X is a bivalent residue derived from optionally substituted thiazole; Y is a bond, lower alkylene or -COHN-; and Z is a groupe of the formulae (II) or (III) wherein R2 is a specified substituent or a pharmaceutically acceptable salt thereof useful as a vascular adhesion protein-1 (VAP-1) inhibitor for preventing or treating a VAP-1associated disease, especially macular edema.
[EN] HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS<br/>[FR] DÉRIVÉS D'AMIDE HÉTÉROCYCLIQUE COMME ANTAGONISTES DU RÉCEPTEUR P2X7
申请人:ACTELION PHARMACEUTICALS LTD
公开号:WO2013108227A1
公开(公告)日:2013-07-25
The invention relates to heterocyclic amide derivatives of formula (I), wherein R1, R2, R3, X and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.
HETEROCYCLIC AMIDE DERIVATIVES AS P2X7 RECEPTOR ANTAGONISTS
申请人:ACTELION PHARMACEUTICALS LTD
公开号:US20150025075A1
公开(公告)日:2015-01-22
The invention relates to heterocyclic amide derivatives of formula (I),
wherein R
1
, R
2
, R
3
, X and n are as defined in the description, their preparation and their use as pharmaceutically active compounds.