首页> 外国专利> PRODUCTON OF ENANTIOMERICALLY PURE 1,3-IMIDAZOLIDINE-4-ONE, ALPHA-AMINO ACID OF ENANTIOMERICALLY PURE BRANCHED OR NONBRANCHED PROTEIN OR NONPROTEIN, AND PEPTIDE AND AMINO ACID MIXTURE CONTAINING ALPHA-AMINO ACID

PRODUCTON OF ENANTIOMERICALLY PURE 1,3-IMIDAZOLIDINE-4-ONE, ALPHA-AMINO ACID OF ENANTIOMERICALLY PURE BRANCHED OR NONBRANCHED PROTEIN OR NONPROTEIN, AND PEPTIDE AND AMINO ACID MIXTURE CONTAINING ALPHA-AMINO ACID

机译:对映体纯的1,3-咪唑啉-4-一,对映体纯的支链或非支链蛋白质或非蛋白质的α-氨基酸,以及含有α-氨基酸的肽和氨基酸混合物的生产

摘要

2.1. The said compounds are to be prepared as economically and cleanly as possible. Depending on the costs of the starting compounds, an optimisation should be possible with respect to the necessary process steps, the yield and/or the purity. Complicated process steps such as extractions and problematical solvents such as dichloromethane should particularly be dispensed with. 2.2. The 1,3-imidazolidin-4-ones of the general formula IMAGE are obtained pure in their preparation, in particular by precipitation, it being possible to employ an optically active acid to 0.5 - 0.8 eq for resolving the racemate. The undesired enantiomer can be racemised in an inert solvent, and the cyclisation to the imidazolidinone can even be carried out by means of the optically active acid, after which the resolution of the racemates takes place directly. 2.3. The 1,3-imidazolidin-4-ones are useful starting materials for the preparation of branched or unbranched, proteinogenic or non-proteinogenic alpha -aminoacids by means of diastereoselective alkylation and subsequent ring cleavage.
机译:2.1。所述化合物应尽可能经济和清洁地制备。取决于原料化合物的成本,关于必要的工艺步骤,产率和/或纯度的优化应该是可能的。尤其应避免使用复杂的处理步骤(例如萃取)和有问题的溶剂(例如二氯甲烷)。 2.2。通式的1,3-咪唑啉丁-4-酮是纯净地制备的,特别是通过沉淀获得的,可以使用旋光酸至0.5-0.8eq来拆分外消旋体。不需要的对映异构体可以在惰性溶剂中外消旋,并且甚至可以通过旋光性酸环化成咪唑烷酮,然后直接消旋外消旋体。 2.3。 1,3-咪唑啉丁-4-酮是有用的起始原料,用于通过非对映选择性烷基化和随后的环裂解制备支链或直链,蛋白质或非蛋白质的α-氨基酸。

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