4-羟基-3-甲氧基苄醇置于palladium Diacetate Tentagel-N(R)C(O)Ch2C2F4oc2F4So2F,Potassium Carbonate,甲酸,1,3-双(二苯基膦)丙烷,三乙胺体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 2.0H,以86%的收率获得产物间甲氧基苯甲醇 参考文献:A Traceless Perfluoroalkylsulfonyl (Pfs) Linker For The Deoxygenation Of Phenols 标题:A Traceless Perfluoroalkylsulfonyl (Pfs) Linker For The Deoxygenation Of Phenols 摘要:[graphics]The Synthesis Of A Novel Perfluoroalkylsulfonyl (Pfs) Fluoride Is Described For Use As A Traceless Linker In Solid-Phase Organic Synthesis. Attachment To The Resin And Subsequent Coupling Of A Phenol Affords A Stable Arylsulfonate That Behaves As A Support-Bound Aryl Triflate. Palladium-Mediated Reductive Cleavage Of A Wide Variety Of Phenols Generated The Parent Arenes. The Resin-Bound Aryl Triflate Was Shown To Be Stable To Reductive Amination Conditions,And The Traceless Synthesis Of Meclizine Is Reported. DOI:10.1021/ol0163732
专利号:US-6765117-B2 优先权日:1997-10-24 标题:Process for stereoselective synthesis of prostacyclin derivatives 发明人:MORIARTY ROBERT M; PENMASTA RAJU; GUO LIANG; RAO MUNAGALA S; STASZEWSKI JAMES P 权利人:UNITED THERAPEUTIC CORP 摘要:An improved method is described for making 9-deoxy-PGF 1 -type compounds. In contrast to the prior art, the method is stereoselective and requires fewer steps than the known methods for making these compounds. The invention also relates to novel intermediates prepared during the synthesis of the 9-deoxy-PGF 1 -type compounds.
专利号:US-2014142279-A1 优先权日:2012-09-13 标 题:Method for peptide synthesis 发明人:LALEZARI IRAJ; LALEZARI PARVIZ 权利人:LALEZARI IRAJ; LALEZARI PARVIZ 摘要:A new method based on the synthesis and use of novel N and C protecting agents. The new N-protecting agent, here referred to as V-Phenol, generates V-protected amino acids and can be successfully applied to all conventional peptide bond formations including active esters, N,N′-dicyclohexylcarbodiimide (DCC) or related dehydrating agents mixed anhydride methods, PC13 and related agents. The new C-protecting agent, here referred to as HONE, can be successfully applied to peptide synthesis as an active ester not only in combination with V-protected amino acids but also with other N-protecting agents such as Cbz, Boc, Fmoc, etc.
专利号:US-12145139-B2 优先权日:2016-02-09 标题 :Manganese based complexes and uses thereof for homogeneous catalysis 发明人:MILSTEIN DAVID; NERUSH ALEX; VOGT MATTHIAS; MUKHERJEE ARUP; ESPINOSA-JALAPA NOEL ANGEL; CHAKRABORTY SUBRATA 权利人:YEDA RES & DEV; NERUSH ARKADI 摘要:The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) C—C coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. (12) preparation of amides (including formamides, cyclic dipeptides, diamide, lactams, polypeptides and polyamides) by dehydrogenative coupling of alcohols and amines; (13) preparation of imides from diols.
专利号:US-2002173672-A1 优先权日:1997-10-24 标 题:Process for stereoselective synthesis of prostacyclin derivatives
专利号:US-8080404-B1 优先权日:2005-04-05 标题:Enzymatic decontamination 发明人:TURETSKY ABRAHAM L; PAWLOWSKI DAVID R; BRICKHOUSE MARK D 权利人:TURETSKY ABRAHAM L; PAWLOWSKI DAVID R; BRICKHOUSE MARK D; US ARMY 摘要:Compositions and methods for enzymatic decontamination by inactivation of Hazardous agents are provided. Hazardous agents of microbial and chemical origin can be neutralized by H 2 O 2 . The methods described herein provide for enzymatic production of H 2 O 2 in situ using oxidoreductase enzymes that use oxygen as an acceptor and their alcohol substrates. The enzymatically produced H 2 O 2 and corresponding aldehydes have potent antimicrobial properties. The enzymatically produced H 2 O 2 also can detoxify chemical agents in situ. The decontaminating power of the oxidoreductase enzymes that use oxygen as an acceptor may be amplified by addition of reagents, such as acetyl donors or base catalysts that, in the presence of H 2 O 2 , yield peroxy acid derivatives and hydroperoxy anions. Such derivatives can neutralize biological and chemical agents, thus providing a broadly applicable decontamination method. In addition, catalytic production of H 2 O 2 in situ results in controlled synthesis of decontamination reagents at their point of use, mitigating the need to store, transport and dispose of hydrogen peroxide solutions in the field.
专利号:US-5659061-A 优先权日:1995-04-20 标 题:Tumor protease activated prodrugs of phosphoramide mustard analogs with toxification and detoxification functionalities 发明人:GLAZIER ARNOLD 权利人:DRUG INNOVATION & DESIGN INC 摘要:The composition, synthesis, and applications of tumor associated protease activated prodrugs of phosphoramide mustard, isophosphoramide mustard and analogs with detoxification functionalities are described. These drugs release a cytotoxic phosphoramide mustard analog following activation by tumor associated proteases and esterases. The general structure for these drugs is: ##STR1## Wherein R1 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; wherein X is a good leaving group such as a halogen; R2 is a beta-X-ethyl-amino group which may optionally bear substituents on the nitrogen or carbon atoms; or an amino group (NH 2 ) which may optionally be substituted. Wherein A is a benzyloxy derivative with one or more acyloxy or acylamino groups in para or ortho portions relative to the phosphoester; and wherein the acyloxy or acylamino groups are not (substituted or unsubstituted) p-guanidino-benzoyloxy groups or p-guanidino-benzoylamino groups.