摘要:
The present invention discloses a method comprising the steps of; a) forming in an aqueous solution a hydroxamic acid from a hydroxylamine free base and anhydride having the formula (RCO).sub.2 O wherein R is H or a substituted or unsubstituted C.sub.2-6 alkyl, C.sub.2-6 alkenyl, C.sub.6-10 aryl, or C.sub.4-10 heteroaryl; and b) treating said hydroxamic acid with an alkylating agent in the presence of at least one proton scavenger under conditions sufficient to consume substantially all of said alkylating agent to form an O-substituted hydroxamate. The protection and alkylation are readily effected in water (with no alcohol co-solvent) without the need for phase-transfer catalysis and with little hydrolysis of the alkylating agent.
摘要:
Esters of 4,5-disubstituted-oxy-2-methyl-3,6-dioxo-cyclohexa-1,4-dienyl alkyl acids were prepared chemically and/or enzymatically. Depending upon the ester, improved melanocyte cytotoxicity was achieved. Improved cytotoxicity characteristics are consistent with ester analogs being more physiologically compatible and less irritating to skin than their corresponding acids.
摘要:
Disclosed are esters and a process for the preparation of the esters represented by formula 1: The process includes reacting an alcohol with a long-chain acid R2COOH or long-chain ester R2COOR4 in the presence of an organic solvent and an enzyme with or without the removal of water.
摘要:
Method for the preparation of ester compounds for use as skin brightening agents and compositions for brightening skin containing the ester compounds.
摘要:
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.
摘要:
Disclosed are novel phosphine-phosphoramidite compounds which may be employed in combination with a catalytically-active metal to effect a wide variety of reactions such as asymmetric hydrogenations, asymmetric reductions, asymmetric hydroborations, asymmetric olefin isomerizations, asymmetric hydrosilations, asymmetric allylations, asymmetric conjugate additions, and asymmetric organometallic additions. Also disclosed are a process for the preparation of the phosphine-phosphoramidite compounds, metal complex compounds comprising at least one of the phosphine-phosphoramidite compounds and a catalytically-active metal and hydrogenation processes utilizing the metal complex compounds.
摘要:
The present invention relates to highly enantiomerically pure lactam-substituted propanoic acid derivatives and methods of making and using therefor. The invention involves a multi-step synthesis to produce the lactam compounds. In one step of the reaction sequence, asymmetric hydrogenation of a lactam-enamide was performed to produce an intermediate that can ultimately be converted to a series of pharmaceutical compounds. The invention also contemplates the in situ synthesis of an intermediate of the multi-step synthesis, which provides economic advantages to the overall synthesis of the lactam compounds.
摘要:
Disclosed are novel phosphinometallocenylamides that are useful as ligands for asymmetric catalysis. The novel ligands, which are readily modifiable, contain both a phosphine and an amide functionality linked by a metallocene backbone. In addition, the novel compounds are phosphine-amides derived from a phosphine-amine, rather than a phosphine-carboxylic acid. Further, described herein are both processes to make the novel ligands as well as processes that employ such ligands in a catalytically active composition comprising one or more phosphinometallocenylamide compounds in complex association with one or more Group VIb or Group VIII metals to provide chiral products. Further, we describe exemplary catalyst complexes incorporating the novel ligands.