CAS: 441045-17-6; (2R,3R,3As,7R,8As,9S,10Ar,11S,12R,13Ar,13Bs,15S,18S,21S,24S,26R,28R,29As)-2-[(2S)-3-Amino-2-Hydroxypropyl]Hexacosahydro-3-Methoxy-26-Methyl-20,27-Bis(Methylene)-11,15:18,21:24,28-Triepoxy-7,9-Ethano-12,15-Methano-9H,15H-Furo[3,2-I]Furo[2',3':5,6]Pyrano[4,

艾瑞布林中间体置于吡啶,2,4,6-三甲基吡啶,Ammonium Hydroxide,氨体系中,用 二氯甲烷,异丙醇,乙腈 作为反应溶剂,化学反应 38.5H,反应生成 甲磺酸艾日布林
参考文献:甲磺酸艾日布林的合成
标题:甲磺酸艾日布林的合成
摘要:本发明涉及甲磺酸艾日布林的合成.具体为提供一种制备甲磺酸艾日布林制备的方法,该方法可以规避专利中usre46965E提及的二聚杂质(Dimer杂质)的产生.

专利信息

专利号:US-11542269-B2
优先权日:2018-01-03
标 题:Prins reaction and compounds useful in the synthesis of halichondrin macrolides and analogs thereof
发明人：CHOI HYEONG-WOOK; FANG FRANCIS G
权利人:EISAI R&D MAN CO LTD
摘要:The invention provides methods utilizing Prins reaction in the preparation of compounds that may be useful as intermediates in the synthesis of halichondrin macrolides and analogs thereof. The invention also provides compounds that may be useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.

专利号:US-11976081-B2
优先权日:2019-04-26
标题 :Intermediate of eribulin and synthesis method and use thereof
发明人：XU WEIPING
权利人:BEIJING TIENYI LUFU PHARMATECH CO LTD
摘要:An intermediate compound is prepared and used for the synthesis of halichondrin B, eribulin or an analog thereof, particularly a structural fragment C27-C35 thereof. The starting materials of the synthetic route are readily available, and the optical purity of the starting materials can be ensured, so that the optical purity of the structural fragment C27-C35 in halichondrin B, eribulin or the analog thereof is ensured. Steps for constructing a chiral center of the structural fragment C27-C35 feature higher diastereoselectivity and yield, in particular preparation methods of compounds of formulae (X), (XI), (XVI) and (XV). By-products of partial reactions can be removed only by recrystallization, which results in easy purification and significant reduce in cost.

专利号:US-11447499-B2
优先权日:2019-06-14
标 题:Process for the preparation of eribulin mesylate intermediate
发明人：KOVI RAVISHANKER; KANNAPPAN JAYARAMAN; PATIL SHIVNATH SAHEBRAO
权利人:RK Pharma Solutions LLC; RK PHARMA INC
摘要:The present application provides improved processes for the synthesis of eribulin intermediate, which generally comprise the steps of: a) De-protecting the eribulin-enone (compound 1) in tetrahydrofuran by using TBAF solution, buffered with imidazole HCl in the presence of molecular sieve and sodium sulphate to get an insitu mixture of eribulin-dione diastereomer at C12 carbon (compound 2). Then ketalization may be performed of eribulin-dione insitu intermediate containing mixture of diastereomer at C12 carbon (compound 2) with PPTS in dichloromethane to yield eribulin-diol (compound 3).

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.

专利号:US-12247239-B2
优先权日:2019-06-21
标题:Chemo-enzymatic process for the preparation of homopropargylic alcohol
发明人：CHANDRASEKHAR SRIVARI; GHOSH SUBHASH; KRISHNA AVULA SHIVA; REDDY CHADA RAJI; SUDHAKAR GANGARAJULA; THENKRISHNAN KUMARAGURU; PABBARAJA SRIHARI; MAINKAR PRATHAMA SATYENDRA; NASAM RAJESH
权利人:COUNCIL SCIENT IND RES; COUNCIL SCIENT IND RES
摘要:The present invention relates to an enzymatic process for preparation of optically pure enantiomers of homopropargylic alcohol compounds of formula I, which are useful intermediates for the synthesis of Halichondrin B and analogs. wherein, P is H or an alcohol protecting group, n is an integer ranging from 0-12.

专利号:US-11697655-B2
优先权日:2021-06-08
标 题 :Synthesis of eribulin mesylate
发明人：QIU XIAOLONG; XU TAO; ZUO ZHIWEI; GE JIE; LU XINWEI; CHU LINGLING; LIU WENBO; WANG BIAO; GU TINGWEI; WANG WEIWEI; HU LIN; ZOU PING; CHEN JUN; CAO LEI
权利人:WISDOM PHARMACEUTICAL CO LTD
摘要:A preparation method of an intermediate compound of formula II ((1R,2S,3S,4S,5S,6R,11S,14S,17S,19R,21R,23S,25R,26R,27S,31R,34S)-25-[(2S)-2,3-dihydroxy]-2,5-dihydroxy-26-methoxy-19-methyl-13,20-dimethylene-24,35,36,37,38,39-hexaoxane[29.3.1.13,6.14,34.111,14.117,21.023,27]nonatriacontan-8,29-dione) for eribulin mesylate is provided, including subjecting a compound of formula I to a reaction with an additive in the presence of tetra-n-butylammonium fluoride (TBAF). The additive is piperidine hydrochloride or pyridine hydrochloride, and a reaction formula is as follows:The present invention aims to avoid the problem that a traditional synthetic route has a low yield.