Invention Grant
- Patent Title: Process for phosphonic ethylation of amines
- Patent Title (中): 氨基磷酸化方法
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Application No.: US3560494DApplication Date: 1966-10-18
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Publication No.: US3560494APublication Date: 1971-02-02
- Inventor: COPP FREDERICK CHARLES
- Applicant: BURROUGHS WELLCOME CO
- Assignee: Glaxo Wellcome Inc
- Current Assignee: Glaxo Wellcome Inc
- Priority: GB3128765 1965-10-22
- Main IPC: C07F9/54
- IPC: C07F9/54 ; C07D87/26
Abstract:
A METHOD FOR PREPARING THE CATION OF FORMULA 1
Z=N-CH(-R5)-CH(-R4)-P(+)(-R1)(-R2)-R3
WHICH COMPRISES REACTING A CATION OF FORMULA II
Q-CH(-R5)-CH(-R4)-P(+)(-R1)(-R2)-R3
WITH A SECONDARY AMINE Z=NH; WHERE R1,R2 AND R3 ARE LOWER ALKYL OR PHENYL. R4 IS HYDROGEN, R5 IS HYDROGEN OR LOWER ALKYL, Q IS PHENOXY UNSUBSTITUTED OR SUBSTITUTED WITH LOWER ALKYL, LOWER ALKOXY OR HALOGENO, Z=N- IS UNSUBSTITUTED DI-LOWER ALKYLAMINO, PYRROLIDINO, MORPHOLINO OR PIPERIDINO, IN ALL DEFINITIONS ABOVE LOWER ALKYL AND LOWER ALKOXY HAVE 1 TO 5 CARBONS. THE PRODUCTS OF THIS METHOD ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF WELL KNOWN ANTIHISTIMINES AND ANALGESICS.
Z=N-CH(-R5)-CH(-R4)-P(+)(-R1)(-R2)-R3
WHICH COMPRISES REACTING A CATION OF FORMULA II
Q-CH(-R5)-CH(-R4)-P(+)(-R1)(-R2)-R3
WITH A SECONDARY AMINE Z=NH; WHERE R1,R2 AND R3 ARE LOWER ALKYL OR PHENYL. R4 IS HYDROGEN, R5 IS HYDROGEN OR LOWER ALKYL, Q IS PHENOXY UNSUBSTITUTED OR SUBSTITUTED WITH LOWER ALKYL, LOWER ALKOXY OR HALOGENO, Z=N- IS UNSUBSTITUTED DI-LOWER ALKYLAMINO, PYRROLIDINO, MORPHOLINO OR PIPERIDINO, IN ALL DEFINITIONS ABOVE LOWER ALKYL AND LOWER ALKOXY HAVE 1 TO 5 CARBONS. THE PRODUCTS OF THIS METHOD ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF WELL KNOWN ANTIHISTIMINES AND ANALGESICS.
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