研究了单齿亚磷酸酯配体三亚磷酸三-1-萘酯P(ONp)3的铑配合物催化的乙酸乙烯酯的区域选择性加氢甲酰化反应。P(ONp)3配体对乙酸乙烯酯加氢甲酰化的速率和选择性表现出相当大的影响,特别是高周转频率(高达11,520 h -1),对优选的支链醛具有极佳的区域选择性(99%),对乙酸的选择性高。醛(93%)。底物对加氢甲酰化反应的活性较低,并且配体(由廉价的化合物1-萘酚合成)易于接近,具有显着的效果,使该系统非常具有吸引力。
Industrially important triaryl phosphites, traditionally prepared from PCl3, have been synthesized by a diphenyl diselenide-catalyzed one-step procedure involving white phosphorus and phenols, which provides a halogen- and transition metal-free way to these compounds. Subsequent oxidation of triaryl phosphites produces triaryl phosphates and triaryl thiophosphates. Phosphorotrithioates are also prepared
Processes for the preparation of 0-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182
申请人:Xu Guoyou
公开号:US20070207972A1
公开(公告)日:2007-09-06
The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a). In particular, the present invention relates to processes and intermediates for the preparation of O-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine:
6-O-substituted erythromycin derivatives having improved gastrointestinal tolerance
申请人:Ma Zhenkun
公开号:US20060166906A1
公开(公告)日:2006-07-27
Compounds having formula (I)
are useful for treating bacterial infections while avoiding the concomitant liability of gastrointestinal intolerance. Compositions containing the compounds and methods of treatment using the compounds are also disclosed.
[EN] BRIDGED MACROCYCLIC COMPOUNDS AND PROCESSES FOR THE PREPARATION THEREOF<br/>[FR] COMPOSES MACROCYCLIQUES PONTES ET PROCEDES DE PREPARATION DESDITS COMPOSES
申请人:ENANTA PHARM INC
公开号:WO2005080408A1
公开(公告)日:2005-09-01
The present invention provides a method for preparing bridged macrocyclic compounds comprising the step of reacting a macrocyclic compound characterized by having at least two nucleophilic moieties with a bifunctional bridging reagent optionally in the presence of a catalyst, thereby producing a bridged macrocyclic product.
[EN] PROCESS FOR THE PREPARATION OF T-11 BICYCLIC ERYTHROMYCIN DERIVATIVES<br/>[FR] PROCEDE DE PREPARATION DE DERIVES BICYCLIQUES 6-11 D'ERYTHROMYCINE
申请人:ENANTA PHARM INC
公开号:WO2005070918A1
公开(公告)日:2005-08-04
The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivatives. In particular, the presen tinvention relates to processes and intermediates for the preparation of a compound of formula (IX-c).