Consecutive Michael-Claisen Process for Cyclohexane-1,3-dione Derivative (CDD) Synthesis from Unsubstituted and Substituted Acetone
摘要:
A long-existing problem of cyclohexane-1,3-dione derivatives (CDD) synthesis from unreactive acetone through consecutive Michael-Claisen process was solved under this study. The practical applicability of this process was tested for a novel compound ethyl 3-(2,4-dioxocyclohexyl) propanoate for up to 20-gram scale. Furthermore, the scope of different acetone derivatives was investigated and resulted with similar consecutive Michael-Claisen process for CDD synthesis. The reaction exhibited remarkable regioselectivity in Michael addition followed by Claisen cyclization. In this process high substrate selectivity was observed for CDD synthesis following consecutive double-Michael-Claisen and Michael-Claisen cyclization.
[EN] NITRILE COMPOUND AND ITS USE IN PEST CONTROL<br/>[FR] COMPOSE NITRILE ET SON UTILISATION POUR LE CONTROLE DES INSECTES ET ANIMAUX NUISIBLES
申请人:SUMITOMO CHEMICAL CO
公开号:WO2005063694A1
公开(公告)日:2005-07-14
The present invention provides a nitrile compound represented by the formula (I): wherein R represents C1-C4 fluoroalkyl, Q represents halogen, C1-C11 alkyl optionally substituted with halogen, C2-C6 alkenyl group optionally substituted with halogen, C2-C6 alkynyl optionally substituted with halogen, C3-C7 cycloalkyl optionally substituted with halogen or (C3-C7 cycloalkyl optionally substituted with halogen)C1-C4 alkyl, which has excellent control effect against pests.
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are 3-imidazoyl-pyrazolo[3,4-b]pyridine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally monocyclic and bicyclic compounds and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.
Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are diazole lactam derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated disease, and as controls in assays for the identification of competitive CCR1 antagonists.
[EN] ORAL COMPLEMENT FACTOR D INHIBITORS<br/>[FR] INHIBITEURS ORAUX DU FACTEUR D DU COMPLÉMENT
申请人:BIOCRYST PHARM INC
公开号:WO2021072198A1
公开(公告)日:2021-04-15
Disclosed are compounds of formula (I), and pharmaceutically acceptable salts thereof, which are inhibitors of the complement system. Also provided are pharmaceutical compositions comprising such a compound, and methods of using the compounds and compositions in the treatment or prevention of a disease or condition characterized by aberrant complement system activity.