4,6-二氯-2,5-联苯嘧啶,氢化奎尼定置于氢氧化钾,Potassium Carbonate体系中,用 甲苯 用作溶剂,化学反应生成(Dhqd)2吡啶 参考文献:Improved Enantioselectivity In Asymmetric Dihydroxylations Of Terminal Olefins Using Pyrimidine Ligands 标题:Improved Enantioselectivity In Asymmetric Dihydroxylations Of Terminal Olefins Using Pyrimidine Ligands 摘要:Bis-Cinchona Alkaloid Substituted Pyrimidine Ligands Were Found To Give Improved Enantioselectivity In The Osmium-Catalyzed Asymmetric Dihydroxylation (Ad) Of Monosubstituted Terminal Olefins. Doi:10.1021/jo00067A002
专利信息
专利号:US-6252079-B1 优先权日:1993-06-30 标 题 :Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; BOM DAVID 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of irinotecan and derivative compounds which comprises of a novel 4+1 radical annulation wherein the precursoris reacted with an aryl isonitrile having the formulawherein X is Br or I, and R4 is an alkyl group, an allyl group, a propargyl group or a benzyl group, and R16 is H, a C1-C6 alkoxy group, agroup wherein p is an integer between 4 and 12, or a C1-C12 acyclic dialkylamino group. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
专利号:US-6982333-B2 优先权日:1993-06-30 标 题:Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof 发明人:CURRAN DENNIS P; JOSIEN HUBERT; KO SUNG BO 权利人:UNIV PITTSBURGH 摘要:The present invention provides a short, convergent total synthesis of camptothecin and related compounds which consists of a novel 4+1 radical annulation. The present invention also provides novel chemical intermediates for such 4+1 radical annulations.
专利号:WO-9516049-A1 优先权日:1993-12-08 标题 :Catalytic chemo-enzymatic asymmetric synthesis of carbohydrates 发明人:WONG CHI-HUEY; SHARPLESS BARRY K 权利人:SCRIPPS RESEARCH INST; WONG CHI HUEY; SHARPLESS BARRY K 摘要:A stereoselective synthesis of carbohydrates employs two key stereoselective steps, viz. an osmium-catalyzed asymmetric dihydroxylation (AD) of an alkene to form an aldol intermediate and an aldolase-catalyzed aldol addition reaction wherein the aldol intermediate is elongated by the addition of a ketone. Moreover, ketoses having four new stereocenters can be synthesized without the use of chiral starting materials. The stereoselectivity of the asymmetric dihydroxylation (AD) reaction is determined by the cis or trans (Z or E) stereoisomeric configuration of the alkene and by the choice of AD-mix, i.e., an AD-mix-α or AD-mix-β. The stereoselectivity of the aldolase-catalyzed addition reaction is determined by the choice of aldolase and by the stereochemistry of the aldol intermediate. Four aldolases with broad substrate specificity are sufficient to produce all possible enantiomeric combinations of the two hydroxymethylene stereocenters formed during the aldol addition reaction. Accordingly, a synthetic scheme combining an osmium-catalyzed asymmetric dihydroxylation (AD) reaction and an aldolase-catalyzed aldol addition reaction enables direct access to a wide range of carbohydrate derivatives containing up to four new hydroxymethylene stereocenters.
专利号:EP-1346767-A1 优先权日:2002-03-15 标 题:Multifunctional catalyst useful in the synthesis of chiral vicinal diols and process for the preparation thereof 发明人:CHOUDARY BOYAPATI MANORANJAN; CHOWDARI NAIDU SREENIVASA; MADHI SATEESH; KANTAM MANNEPALLI LAKSHMI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a multifunctional reusable catalyst and to a processnfor the preparation thereof on a single matrix of the support to perform multicomponentnreaction in a single pot. The multifunctional catalysts of the invention are useful for thensynthesis of chiral vicinal diols by tandem and / or simultaneous reactions involving Heckncoupling, N-oxidation and AD reaction of olefins in presence of cinchona alkaloidncompounds both as an native one and immobilized one in the said matrix support. Thisninvention also relates to a process for preparing vicinal diols by asymmetric dihydroxylationnof olefins in presence of cinchona alkaloid compounds employing reusable multifunctionalncatalysts as heterogeneous catalysts in place of soluble osmium catalysts.
专利号:US-2003073840-A1 优先权日:2001-08-27 标 题 :Intermediates and methods of preparation of intermediates in the enantiomeric synthesis of (20R)homocamptothecins and the enantiomeric synthesis of (20R)homocamptothecins
专利号:US-6211371-B1 优先权日:1993-06-30 标 题:Intermediates in the synthesis of camptothecin and related compounds and synthesis thereof