NOVEL INTERMEDIATE FOR CARBAPENEM COMPOUND FOR ORAL ADMINISTRATION AND PROCESS FOR PRODUCING THE SAME

WIPO Patent Application WO/2004/043973

A1

A novel intermediate which is for use in efficiently producing a 1β-methylcarbapenem compound for oral administration; and a process for producing the intermediate. The process, which is for producing a novel β-lactam compound represented by the general formula (4), is characterized by reacting a β-lactam compound represented by the general formula (5) as a starting material with a compound represented by the general formula (6) in the presence of a base to obtain a novel β-lactam compound represented by the general formula (1), protecting the hydroxy group, subsequently cyclizing the protected compound in the presence of a strong base, reacting the cyclized compound with diphenylphosphoryl chloride to obtain a novel β-lactam compound represented by the general formula (3), and removing the protective group therefrom. (5) (6) (1) (3) (4) (In the formulae, R₁ represents trimethylsilyl or triethylsilyl; R₂ represents aryl or heteroaryl; R₃ represents C_1-10 alkyl or C_3-10 cycloalkyl; and X represents halogeno.)

NISHINO KEITA (JP)
KOGA TERUYOSHI (JP)

PCT/JP2003/014419

May 27, 2004

November 13, 2003

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KANEKA CORP (JP)
NISHINO KEITA (JP)
KOGA TERUYOSHI (JP)

C07D205/08; C07D477/18; C07F9/6561; (IPC1-7): C07F9/6561; C07D205/08; C07F7/18; C07F19/00

EP0559533A1

1993-09-08

SAKURAI O. ET AL: "A New Synthesis of 1&1t;SYM98>-Alkylcarbapenems Utilizing Eschenmoser Sulfide Contraction of the Novel Thiazinone Intermediates", JOURNAL OF ORGANIC CHEMISTRY, vol. 61, no. 22, 1996, pages 7889 - 7894, XP002986759
See also references of EP 1582526A4

Yasutomi, Yasuo (4-20 Nishinakajima 5-chome, Yodogawa-k, Osaka-shi Osaka, JP)

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