METHOD FOR PREPARING CEPHALOSPORIN INTERMEDIATES COMPOUNDS USING ALPHA-IODO-1-AZETHIDINE ACETIC ACID ESTERS AND TRIALKYL PHOSPHITES Russian patent published in 2008 - IPC C07D501/00 C07D405/12 C07D501/18 C07D501/20

Abstract RU 2321590 C1

FIELD: organic chemistry, chemical technology.

SUBSTANCE: invention relates to a method for synthesis of compound of the formula (I): wherein R¹ represents para-nitrobenzyl or allyl; X represents halogen atom. Method involves: (1) interaction of compound of the formula (IVa): wherein R¹ represents para-nitrobenzyl or allyl, and R² represents benzyl or substituted benzyl with P(OR³)₃ in a solvent medium to yield compound of the formula (III): wherein R¹ represents para-nitrobenzyl or allyl; R² represents benzyl or substituted benzyl; R³ represents (C₁-C₆)-alkyl and (2) the following heating compound of the formula (III) in a solvent in the presence of LiCl and organic soluble base to form compound of the formula (II): wherein R¹ represents para-nitrobenzyl or allyl; R² represents benzyl or substituted benzyl, and (3) interaction of compound of the formula (II) with R⁴-OH and PX₅ to form compounds of the formula (I) that is an intermediate compound in synthesis of cephalosporin.

EFFECT: improved method of synthesis.

14 cl, 5 ex

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RU 2 321 590 C1

Authors

Morita Khiromasa

Nagakura Isao

Norris Timoti

Dates

2008-04-10—Published

2005-02-25—Filed