Invention Grant
- Patent Title: Phosphono substituted acylpenicillins
- Patent Title (中): 磷酸二氢卟吩
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Application No.: US8701870Application Date: 1970-11-04
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Publication No.: US3828025APublication Date: 1974-08-06
- Inventor: HAMANAKA E
- Applicant: PFIZER
- Assignee: Pfizer
- Current Assignee: Pfizer
- Priority: US8701870 1970-11-04
- Main IPC: C07D499/00
- IPC: C07D499/00 ; C07D499/44 ; C07D99/16
Abstract:
BROAD SPECTRUM ANTIBACTERIAL AGENTS; NAMELY, A-(PHOSPHONOALKYL) AND A-(W-PHOSPHONOCYCLOALKYL)PENICILLINS OF THE FORMULA
2-(R3OOC-),3,3-DI(H3C-),6-(R5-O-P(=O)(-O-R4)-(CH2)N-C(-R1)
(-R2)-CO-NH-)-PENAM
AND THE NON-TOXIC CATIONIC SALTS THEREOF WHEREIN R1 IS HYDROGEN, LOWER ALKYL, PHENYL AND SUBSTITUTED PHENYL WHEREIN THE SUBSTITUENT IS LOWER ALKYL, LOWER ALKOXY, CHLORO, BROMO, FLUORO AND TRIFLUOROMETHYL; R2 IS HYDROGEN; R1 AND R2 TOGETHER WITH THE CARBON ATOM TO WHICH THEY ARE ATTACHED ARE ALICYCLIC OF FROM 3 TO 7 CARBON ATOMS; R3 IS HYDROGEN AND ACYLOXY LOWER ALKYL WHEREIN THE ACYLOXY MOIETY IS LOWER ALKANOYLOXY, BENZOYLOXY AND SUBSTITUTED BENZOYLOXY WHEREIN THE SUBSTITUENT IS CHLORO, BROMO, FLUORO, LOWER ALKYL, LOWER ALKOXY AND TRIFLUOROMETHYL; N IS 0 OR AN INTEGER FROM 1 TO 8; EACH OF R4 AND R5 IS HYDROGEN, LOWER ALKYL, SUBSTITUTED LOWER ALKYL WHEREIN THE SUBSTITUENT IS LOWER ALKOXY AND FLUORO; PHENYL AND SUBSTITUTED PHENYL WHEREIN THE SUBSTITUENT IS CHLORO, BROMO, FLUORO, LOWER ALKYL, LOWER ALKOXY AND TRIFLUOROMETHYL.
2-(R3OOC-),3,3-DI(H3C-),6-(R5-O-P(=O)(-O-R4)-(CH2)N-C(-R1)
(-R2)-CO-NH-)-PENAM
AND THE NON-TOXIC CATIONIC SALTS THEREOF WHEREIN R1 IS HYDROGEN, LOWER ALKYL, PHENYL AND SUBSTITUTED PHENYL WHEREIN THE SUBSTITUENT IS LOWER ALKYL, LOWER ALKOXY, CHLORO, BROMO, FLUORO AND TRIFLUOROMETHYL; R2 IS HYDROGEN; R1 AND R2 TOGETHER WITH THE CARBON ATOM TO WHICH THEY ARE ATTACHED ARE ALICYCLIC OF FROM 3 TO 7 CARBON ATOMS; R3 IS HYDROGEN AND ACYLOXY LOWER ALKYL WHEREIN THE ACYLOXY MOIETY IS LOWER ALKANOYLOXY, BENZOYLOXY AND SUBSTITUTED BENZOYLOXY WHEREIN THE SUBSTITUENT IS CHLORO, BROMO, FLUORO, LOWER ALKYL, LOWER ALKOXY AND TRIFLUOROMETHYL; N IS 0 OR AN INTEGER FROM 1 TO 8; EACH OF R4 AND R5 IS HYDROGEN, LOWER ALKYL, SUBSTITUTED LOWER ALKYL WHEREIN THE SUBSTITUENT IS LOWER ALKOXY AND FLUORO; PHENYL AND SUBSTITUTED PHENYL WHEREIN THE SUBSTITUENT IS CHLORO, BROMO, FLUORO, LOWER ALKYL, LOWER ALKOXY AND TRIFLUOROMETHYL.
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