CAS: 143527-70-2; (4S,5R)-3-(Tert-Butoxycarbonyl)-2,2-Dimethyl-4-Phenyloxazolidine-5-Carboxylic Acid

相似化合物

184363-66-4 223134-87-0 215171-14-5

专利信息

专利号:US-6433180-B1
优先权日:1992-10-30
标 题 :Carboxylic acids for synthesis of taxane derivatives
发明人：DENIS JEAN-NOEL; GREENE ANDREW-ELLIOT; KANAZAWA ALICE
权利人:AVENTIS PHARMA SA
摘要:Novel carboxylic acids of formula (VI), useful for preparing taxane derivatives of general formula (I) by esterifying protected baccatine (III) or protected diacetyl baccatin (III) with an acid of general formula (II). The products of general formula (I) are particularly useful for preparing taxol, Taxotere and analogs thereof having anti-tumor properties.

专利号:WO-2016098015-A1
优先权日:2014-12-16
标题 :New efficient methods for the synthesis of taxane derivatives such as docetaxel and their structural analogous, and a method for the preparation thereof
发明人：KARIMIAN KHASHAYAR; SAFARI HATAM; MOFAKHAM HAMID; NAZARI SABER; EISAPOUR ELIAS; AZIMI HOSEIN ALI; ROSTAMIAN ALI REZA
权利人:KARIMIAN KHASHAYAR
摘要:The present invention relates to a novel process for the preparation of taxanes such as Docetaxel, a very important anticancer drug. Docetaxel 1 is a clinically well-established anti -mitotic chemotherapy medication used mainly for the treatment of breast, ovarian and non-small cell lung cancer. In this work we introduce an efficient and simple process for producing Docetaxel 1 (vide infra), including the following steps: a) hydroxyl acylation reaction of 10-DAB-III with chloroacetic acid to obtaine compound 2; b) condensation reaction of compounds 2 and 3 to obtain compound 4; c) deprotection of protecting group paramethoxy phenyl (PMP) protecting group to obtain compound 5 d) deprotection of protecting group Rl of compound 5 to prepare Docetaxel 1; wherein, Rl is, among other acetylation reagents, chloroacetyl chloride, R2 is, among other ketones and aldehydes, paramethoxy phenyl (PMP), and R3 is, among other alkanes, tert-butyl e) subjecting the crude Docetaxel to fast filtration over a short silica gel filter to obtain anhydrous Docetaxel of > 95% purity f) crystallizing the anhydrous Docetaxel of step e) to obtain pharmaceutical grade Docetaxel trihydrate. In the methods for preparation of the present invention, the protective groups used are easily removed, the purification of the intermediates is convenient, the cost of production is reduced, the steps of reaction are fewer, the yield and the purity are higher, and the processes can be scaled to commercial scale production. Another important aspect of the present invention is the preparation of pharmaceutical grade Docetaxel without resorting to chromatography.

专利号:CN-114751876-A
优先权日:2022-01-24
标题 :Method for the synthesis of cabazitaxel and docetaxel from 9-dihydro-13-acetylbaccatine III

专利号:RU-2119485-C1
优先权日:1992-03-06
标 题 :Derivatives of taxane-iii, methods of their synthesis and a pharmaceutical composition