摘要:
The invention relates to a process for preparing 4-trifluoromethyl methoxyacetophenone comprising: (a) reacting the compound of Formula XIII with the compound of formula XIX to form the product of formula XX: and (b) hydrolyzing the compound of formula XX to 4-trifluoromethyl methoxyacetophenone:
摘要:
A process for preparing an hydroxyketone of the formula (X):
wherein Ar represents substituted phenyl, aromatic heterocyclic, or substituted aromatic heterocyclic; R 1 and R 2 independently represents hydrogen, C-1 to C-16 alkyl, aromatic, substituted aromatic, aromatic heterocyclic, substituted aromatic heterocyclic or C-1 to C-5 alkyl covalently bonded to Ar, with the provision that R 1 and R 2 are different. The process comprises contacting a compound of the formula (V):
with a solvent, a base and a chiral hydroxylating agent at a temperature of about -85°C or less. Compounds of the formulae
also are disclosed.
摘要翻译:制备式(X)的羟基酮的方法:其中Ar表示取代的苯基,芳族杂环或取代的芳族杂环; R 1和R 2独立地表示氢,C 1至C 16烷基,芳族,取代的芳族,芳族杂环,取代的芳族杂环或与Ar共价结合的C-1至C-5烷基, R 1和R 2不同。 该方法包括在约-85℃或更低的温度下使式(V)化合物:与溶剂,碱和手性羟基化试剂接触。 也公开了式的化合物。
摘要:
Bicyclic compounds are disclosed which are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents and in the treatment of hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed. Many of the compounds are novel; inventive methods for their preparation and for the preparation of intermediates, are also disclosed.
摘要:
A process for the preparation of a chiral a-hydroxyketone, or ester thereof, comprising hydrolyzing an ester of said a-hydroxyketone with an enzyme that has a specificity for one enantiomer, or by esterifying said a-hydroxyketone with an esterifying agent in the presence of an enzyme that favors one enantiomer.
摘要:
Bicyclic compounds are disclosed which are useful as anti-allergic, anti-inflammatory and/or cytoprotective agents and in the treatment of hyperproliferative skin disease. Pharmaceutical compositions and methods of treatment employing such compounds are also disclosed. Many of the compounds are novel; inventive methods for their preparation and for the preparation of intermediates, are also disclosed.
摘要:
A process for producing a compound having the formula wherein Pr is hydrogen or a hydroxy protecting group and Pr¹ is a carboxy protecting group, comprising reacting a compound of the formula wherein Pr is as previously defined, with a compound having the formula Pr¹-OH, wherein Pr¹ is as previously defined and either mineral acid or a silver salt of an organic base, and reacting the product so produced with a compound having the formula: wherein L is a leaving group. Three reaction schemes are disclosed as well as novel intermediate compounds.
摘要:
The invention relates to a process for selectively preparing a mono-4-protected 2-methylpiperazine from its corresponding 2-methylpiperazine in high yields, said process comprising reacting said 2-methylpiperazine with about a molar equivalent of a protecting reagent in a solvent, with the reaction being catalyzed by an acid catalyst or a base catalyst.
摘要:
The invention relates to a process for selectively preparing a mono-4-protected 2-methylpiperazine from its corresponding 2-methylpiperazine in high yields, said process comprising reacting said 2-methylpiperazine with about a molar equivalent of a protecting reagent in a solvent, with the reaction being catalyzed by an acid catalyst or a base catalyst.
摘要:
The invention relates to a process for preparing 4-trifluoromethyl methoxyacetophenone comprising: (a) reacting the compound of Formula XIII with the compound of formula XIX to form the product of formula XX:
and (b) hydrolyzing the compound of formula XX to 4-trifluoromethyl methoxyacetophenone: