170985-86-1Relevant articles and documents
Synthetic method of high-purity posaconazole
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Paragraph 0008; 0013-0015, (2020/12/31)
The invention discloses a synthetic method of high-purity posaconazole. The synthetic method comprises the following steps: S1, reacting a compound with a compound 2 to generate a compound 3; S2, removing anisole from the compound 3 under the action of hydrochloric acid to generate a compound required by the patent, namely posaconazole; and S3, carrying out primary refining on the obtained posaconazole crude product to obtain a medicinal high-purity posaconazole finished product.
Preparation method of high-purity posaconazole
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, (2019/06/27)
The invention discloses a preparation method of posaconazole, comprising: subjecting BP004b04 and oxalic acid to salt forming to obtain POE; subjecting POE and di-tert-butyl decarbonate to reaction inthe presence of a base to obtain POP, and recrystallizing POP; subjecting POP and POK o reaction in the presence of a base to obtain POR, and removing tert-butyl carbonate protecting group from POR to obtain POS; subjecting the POS to ring closing to obtain POB; subjecting the POB and POA to reaction to obtain posaconazole. Posaconazole prepared via the preparation method has the content of diastereoisomers being /=0.01%, and the overall route has high total yield.
POSACONAZOLE, COMPOSITION, INTERMEDIATE, PREPARATION METHOD THEREFOR, AND USES THEREOF
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Paragraph 0248-0249, (2019/03/14)
The present invention relates to a compound of formula III, wherein, R is selected from the group consisting of C1-C4 alkyl, substituted or unsubstituted phenyl, and substituted or unsubstituted benzyl, preferably isopropyl; and two Ar groups may be the same or different, and are each independently selected from the group consisting of substituted or unsubstituted aryl groups, preferably substituted or unsubstituted phenyl, such as p-methoxyphenyl and the like, wherein the compound is preferably in a solid form.