PREPARATION METHOD FOR INTERMEDIATE COMPOUND ACTING AS SYNTHETIC POSACONAZOLE, AND INTERMEDIATE COMPOUND PREPARED THEREBY

WIPO Patent Application WO/2023/173717

A1

The present invention relates to a preparation method for an intermediate compound acting as a posaconazole synthetic drug, and an intermediate compound prepared thereby. The preparation method for a compound of formula (I) provided by the present invention comprises: using methyl 4-(2,4-difluorophenyl)-4-enopentanoic acid or a reduction product thereof, i.e. 4-(2,4-difluorophenyl)-4-entenal formaldehyde, as a starting material; firstly, reacting same with formaldehyde or paraformaldehyde in the presence of a chiral catalyst; then performing characteristic oxidation, an esterification reaction and a halogenation cyclization reaction thereon; and finally, performing hydrolysis and an acid treatment. The preparation method in the present invention has the advantages of mild reaction conditions, a simple reaction process, a high total yield and high purity of target products, etc., and is suitable for industrial production.

DAI CHUNGUANG (CN)
ZHU BAOYUN (CN)
ZHANG LIRONG (CN)
PU XUECAN (CN)
YU GUANNENG (CN)
LI YUNFENG (CN)
ZHENG ZHIGUO (CN)

PCT/CN2022/120774

September 21, 2023

September 23, 2022

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ZHEJIANG AUSUN PHARMACEUTICAL CO LTD (CN)

C07D307/24; C07C45/41; C07C49/235; C07C51/31; C07C59/56; C07C67/11; C07C69/732; C07D319/06; C07D405/06

CN105440022A	2016-03-30
CN105503765A	2016-04-20
CN114591272A	2022-06-07

CHINA SCIENCE PATENT & TRADEMARK AGENT LTD. (CN)

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