摘要:
An optically active β-aminocarbonyl compound is obtained by a Mannich reaction between an aldimine in which nitrogen is protected and a malonic acid diester, in the presence of optically active BINOL and dialkyl magnesium (in which two alkyl groups are the same or different) in an amount 1 to 2 molar times the amount of the BINOL.
摘要:
The present invention relates to a process for the preparation of a mixture of aspartic acid diethoxy succinate and an amino acid derivative of the general formula (I) wherein n is 1-10, m is 0 or 1, and R is hydrogen or an alkali metal or alkaline earth metal ion, comprising reacting maleate with diethanol amine under alkaline conditions in the presence of a lanthanoid catalyst to form aspartic acid diethoxy succinate followed by adding aspartic acid which reacts with unreacted maleate to form imino disuccinic acid, i.e. an amino acid derivative of formula (I) wherein m is 0, or by adding a diamine derivative of the general formula (II) NH2(CH2)nNH2 wherein n is as defined above, which reacts with unreacted maleate to form an amino acid derivative of formula (I) wherein m is 1 and n is as defined above.
摘要:
Compounds of formula (I): wherein Ar represents an, optionally substituted, aryl or heteroaryl group, R represents an, optionally substituted, aryl or heteroaryl group, an optionally substituted straight or branched chain C1.10-alkyl, R1 is H or methyl, X is an extender group, n is 0 or an integer between 1 and 12 inclusive, A is a polyol residue wherein the unsubstituted polyol from which the residue is derived has at least y OH groups, and y is an integer>1, can easily be prepared, and are useful as synergists in radiation curing.
摘要:
Methods of preparing NHE-1 inhibitors are disclosed. The NHE-1 inhibitors are useful for the reduction of tissue damage resulting from tissue ischemia.
摘要:
An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
摘要:
An imine fixed to a resin characterized in that it is represented by the following formula: P-Q-N=CH-R wherein P represents a main chain of a polymer constituting the resin, Q represents a hydrocarbon side chain optionally substituted with a substituent which may be bonded via a heteroatom and R represents an optionally substituted hydrocarbon group or a heterocyclic group, and a β-aminocarbonyl compound fixed to a resin represented by formula (II) are provided. The β-aminocarbonyl compound fixed to a resin is a β-aminocarbonyl compound being handled in a solid form. An amine fixed to a resin which is a key compound for a solid state synthesis of this type and represented by the following formula: P-Q1-O-Q2-NH2, wherein Q1 and Q2 are each a hydrocarbon chain selected from among an arylene group, an alkylarylene group and an arylenealkylene group, is also provided, which allows the synthesis of β-aminocarbonyl compound by application of an iminoaldol reaction in a solid phase.
摘要:
This invention relates to methods for making oxetan-3-ylmethanamines having the formula (I) wherein R1? and R2? are as defined herein. The methods of the invention provide the compounds of formula (I) in high yields and under conditions amenable for large-scale commercial production.