📜(S)-(-)-α-甲氧基-α-(三氟甲基)苯乙酸 反应生成(R)-(-)-α-甲氧基-α-(三氟甲基)苯乙酰氯 参考文献:Baudouy,Rene;Maliverney,Christian,Tetrahedron,44,(1988) N 2,471-480 标题:Baudouy,Rene;Maliverney,Christian,Tetrahedron,44,(1988) N 2,471-480
专利号:US-6849743-B2 优先权日:1997-08-15 标 题 :Synthesis of clasto-lactacystin β-lactone and analogs thereof 发明人:SOUCY FRANCOIS; FLAMONDON LOUIS; BEHNKE MARK; ROUSH WILLIAM 权利人:MILLENNIUM PHARM INC 摘要:The present invention is directed to an improved synthesis of clasto-lactacystin-β-lactone, and analogs thereof, that proceeds in fewer steps and in much greater overall yield than syntheses described in the prior art. The synthetic pathway relies upon a novel stereospecific synthesis of an oxazoline intermediate and a unique stereoselective addition of a formyl amide to the oxazoline. Also described are novel clasto-lactacystin-β-lactones, and analogs thereof and their use as proteasome inhibitors.
专利号:US-7423154-B2 优先权日:2001-03-07 标 题 :Asymmetric process for the preparation of diarylethylpiperazines derivatives and novel asymmetric diarylmethylamines as intermediates 发明人:BROWN WILLIAM; PLOBECK NIKLAS 权利人:ASTRAZENECA AB 摘要:An asymmetric synthesis of diarylmethylpiperazines is described. The synthetic route enables preparation of a variety of enatiomerically pure amines with different N-alkyl groups. The invention includes an asymmetric addition of organometallic compounds to chiral sulfinimine to give adducts in predominantly one diastereomer can subsequently be transferred into pure enantiomers of by cleavage of the chiral auxilliary which is followed by synthesis of the piperazine ring by alkylation procedures.
专利号:US-2016318862-A1 优先权日:2013-09-25 标 题:Synthesis of delta 12-pgj3 and related compounds 发明人:NICOLAOU KYRIACOS C; HERETSCH PHILIPP; HALE CHRISTOPHER R H; EL GHZAOUI ABDELLATIF EL MARROUNI; PULUKURI KIRAN KUMAR; YU RUOCHENG; GROVE CHARLES 权利人:UNIV RICE WILLIAM M 摘要:In one aspect, the present invention provides novel derivatives of Δ 12 -PGJ 3 and modular synthetic pathways to obtaining Δ 12 -PGJ 3 and derivatives thereof. In some aspects, the present derivatives of Δ 12 -PGJ 3 are useful as chemotherapeutic agents. The present disclosure also describes compositions of these derivatives as well as methods of use of the derivatives thereof.
专利号:US-4952710-A 优先权日:1988-10-07 标 题:Cyclopenteneheptenoic acid derivatives and method of preparation thereof 发明人:BABIAK KEVIN A; CAMPBELL ARTHUR L 权利人:SEARLE & CO 摘要:This invention relates to a novel cyclopenteneheptenoic acid derivative having the following formula wherein R1 is hydrogen, -COCH3, -COCF3, -CO-phenyl, or a hydroxyl protecting group such as tetrahydropyranyl, tetrahydrofuranyl, or tri-lower alkylsilyl; wherein R2 is -CH2OR1, -COOH, -COOR, -CHO, -CH2-OSi(R12)3, wherein R is lower alkyl and each R12 is independently lower alkyl or aryl; and wherein Y is ethylene, cis-vinylene, trans-vinylene, or acetylene. Also disclosed is a novel process for preparation of the above-defined cyclopenteneheptenoic acid derivative. This process involves coupling of a higher order cuprate complex with a chiral cyclopentene compound. The resultant product is particularly useful as a starting compound for high yield synthesis of optically active prostaglandins.
专利号:US-5486625-A 优先权日:1994-07-08 标 题:Process for the preparation of chiral intermediates useful for the synthesis of antifungal agents 发明人:LEONG WILLIAM; SMITH LYMAN H 权利人:SCHERING CORP 摘要:Described is a process for preparing chiral compounds of the formula ##STR1## wherein X 1 and X 2 are independently F or Cl, and Y is Cl, Br or I, comprising reacting a triol of the formula ##STR2## wherein X 1 and X 2 are as defined above, with acetone in the presence of a catalyst, then with a halogen selected from Cl 2 , Br 2 or I 2 , or N-bromosuccinimide or N-iodosuccinimide.
专利号:US-2003191322-A1 优先权日:1997-08-15 标题:Synthesis of clasto-lactacystin beta-lactone and analogs thereof
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 247. 参考文献:10.1007/s10529-008-9747-9 摘要:Miyazawa T, Houhashi M, Inoue Y, Murashima T, Yamada T. Resolution of secondary alcohols via Carica papaya lipase-catalyzed enantioselective acylation. Biotechnol Lett. 2008 Oct;30(10):1783–7. doi: 10.1007/s10529-008-9747-9.