MORPHOLINE DERIVATIVE

• Main Author: OTA SHUNSAKU
• Format: Patent
• Language: English
• Published: 14.09.1998
• Edition: 6
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS; TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE

PROBLEM TO BE SOLVED: To obtain the subject new compound useful as an intermediate for α-amino acids such as a β-hydroxy-α-amino acid. SOLUTION: This compound is represented by formula I (R1 , R2 and R3 are each H or an alkyl; R4 is H, an alkyl or an amino-protecting group; R5 is H or a substitutable alkyl, except that both R1 and R2 are H and one of R1 and R2 is H and the other is methyl), e.g. 6-tert-butylmorpholine-2,5-dione. The compound represented by formula I (in which R5 is a substitutable alkyl) is obtained by passing a carbonyl compound as a starting raw material through 6 steps such as cyanation, hydrolysis, condensation and deprotection, converting the carbonyl compound into a compound represented by formula II and then reacting the resultant compound represented by formula II with a halide compound. An α-amino acid is simply obtained by hydrolyzing the compound represented by formula I. The compound represented by formula I is good in crystallinity, provides a stable synthetic raw material for the α-amino acid, especially serine, threonine, etc., and is useful as a therapeutic agent for Parkinson's disease.