2-亚甲基丙烷-1,3-二基二乙酸酯置于甲醇,Potassium Carbonate体系中,化学反应生成2-亚甲基-1,3-丙二醇 参考文献:Synthesis Of Isofagomine And A New C6 Pyrrolidine Azasugar With Potential Biological Activity 标题:Synthesis Of Isofagomine And A New C6 Pyrrolidine Azasugar With Potential Biological Activity 摘要:描述了一种高效的不对称合成异法戈敏的方法,该方法基于一种含有三个不同羟基功能的前体.在关键的烷基化步骤中,副产物转化为(2S,3R,4R)-2,4-双(羟甲基)-3-羟基吡咯烷,这是一种新的c6吡咯烷氮糖,能够抑制酵母中的α-葡萄糖苷酶. Doi:10.1055/s-2008-1078280
专利号:US-2009247754-A1 优先权日:2008-03-25 标 题:Method of preparing huperzine a and derivatives thereof 发明人:UNDERINER GAIL; GIBSON FRANK; HE LINLI; MEERA HARIHARA SUBRAMANIAN; GNANADEEPAM JESUDOSS MERCY; SAIGANESH RAMANATHAN; TUDHOPE STEPHEN R; AZADI-ARDAKANI MANOUCHEHR 权利人:DEBIOPHARM SA 摘要:The present invention is related to the synthesis of huperzine A. The synthesis includes a variety of process steps that increase productivity, reduce safety concerns, and allow for increasing production of compounds of desired optical isomer. The inventive methods may encompass a single improved reaction step that may be incorporated into a known reaction process for synthesizing huperzine A or a derivative thereof to improve the overall reaction. The inventive methods also encompass complete synthesis methods for preparing huperzine A or a derivative thereof.
专利号:US-2004116724-A1 优先权日:1996-12-06 标 题:Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds 发明人:KINNEY WILLIAM A; JONES STEVEN; ZHANG XUEHAI; RAO MEENA N; BULLIARD MICHEL; MECKLER HAROLD; LEE NANCY 摘要:A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.
专利号:US-7563877-B2 优先权日:2006-03-02 标题 :Processes for the preparation of 0-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine for the synthesis of 6,11-bicyclic erythromycin derivative EDP-182 发明人:XU GUOYOU; GAI YONGHUA; WANG GUOQIANG; OR YAT SUN; WANG ZHE 权利人:ENANTA PHARM INC 摘要:The present invention relates to processes and intermediates for the preparation of 6-11 bicyclic erythromycin derivative known as EDP-182 (IX-a). In particular, the present invention relates to processes and intermediates for the preparation of O-(2-aminobenzo[d]oxazol-5-yl)methyl hydroxylamine:
专利号:US-6610866-B2 优先权日:1996-12-06 标 题 :Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds 发明人:KINNEY WILLIAM A; JONES STEVEN; ZHANG XUEHAI; RAO MEENA N; BULLIARD MICHEL; MECKLER HAROLD; LEE NANCY 权利人:MAGAININ PHARMA 摘要:A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.
专利号:US-9023813-B2 优先权日:2011-04-13 标题:Synthesis and use of glycoside derivatives of propofol 发明人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN 权利人:SHULL BRIAN; BALDWIN JOHN; GOPALASWAMY RAMESH; HAROON ZISHAN; NUTEK PHARMA LTD 摘要:The present invention relates to methods and compositions for the synthesis, production, and use of pro-drug propofol analogs. This invention relates to a method for the production of a broad group of glycosylated propofol carbohydrate derivatives.
专利号:US-2010298504-A1 优先权日:2007-09-19 标题 :Amphiphilic polymer and processes of forming the same 发明人:Janczewski Dominik; TOMCZAK NIKODEM; KHIN YIN WIN; HAN MINGYONG; VANCSO JULIUS 权利人:AGENCY SCIENCE TECH & RES 摘要:Disclosed are an amphiphilic polymer, its synthesis and uses thereof. The polymer has a hydrocarbon backbone with —COOH side groups. It further has first aliphatic moieties with a main chain of about 3 to about 20 carbon atoms and 0 to about 3 heteroatoms, and second aliphatic moieties that have a main chain of about 3 to about 80 carbon atoms and about 2 to about 40 heteroatoms. The second aliphatic moieties have a copolymerisable group. In the synthesis a maleic anhydride polymer of formula (I) where n is an integer from about 10 to about 10000 and R1 is H or methyl, is reacted with a monofunctional compound with an alkyl chain of about 3 to about 20 carbon atoms and 0 to about 2 heteroatoms, and with an at least bifunctional compound with an alkyl chain of about 3 to about 80 carbon atoms and 0 to about 40 heteroatoms. The functional group of the monofunctional compound and one functional group of the at least bifunctional compound can form a linkage with an anhydride. Another functional group of the at least bifunctional compound, which is not allowed to react with the maleic anhydride polymer, is copolymerisable.