专利号:US-7339066-B1 优先权日:2006-05-31 标题 :Intermediates for the synthesis of polypropionate antibiotics 发明人:PARKER KATHLYN; CAO HUANYAN 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The invention relates to intermediate compounds of the formula n nwherein R 1 is H or a protecting group, R 2 and R 3 each independently represent H, methyl, or a leaving group, provided that at least one, but not both, of R 2 and R 3 is a leaving group. The intermediate compounds are useful for the synthesis of discodermolide, its derivatives, and related compounds.
专利号:US-9982005-B2 优先权日:2013-04-04 标 题 :Macrolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing macrolides by the coupling of an eastern and western half, followed by macrocyclization, to provide macrolides, including both known and novel macrolides. Intermediates in the synthesis of macrolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using the inventive macrolides are also provided. A general diastereoselective aldol methodology used in the synthesis of the western half is further provided.
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-11466046-B2 优先权日:2014-10-08 标题 :14-membered ketolides and methods of their preparation and use 发明人:MYERS ANDREW G; SEIPLE IAN BASS; ZHANG ZIYANG 权利人:HARVARD COLLEGE 摘要:Provided herein are methods of preparing new 14-membered ketolides via coupling of an eastern and western half moiety, followed by macrocyclization, and optional functionalization. Intermediates in the synthesis of these ketolides including the eastern and western halves are also provided. Pharmaceutical compositions and methods of treating infectious diseases and inflammatory conditions using these ketolides are also provided.
专利号:US-6552239-B1 优先权日:1999-10-28 标题:Synthesis of cyclopropaneacetylene by a one-pot process 发明人:BRANDS KAREL M J 权利人:MERCK & CO INC 摘要:The present invention relates to a process for the preparation of cyclopropaneacetylene by reacting a ketophosphonate with a diazo-transfer reagent in the presence of non-nucleophilic base in an aprotic solvent to generate a reaction mixture containing a ketodiazophosphonate compound and then reacting the reaction mixture with cyclopropanecarboxaldehyde in a non-nucleophilic base and a protic solvent to yield cyclopropaneacetylene.
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.