专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-7202370-B2 优先权日:2003-10-27 标 题 :Semi-synthesis of taxane intermediates from 9-dihydro-13-acetylbaccatin III 发明人:NAIDU RAGINA 权利人:CONOR MEDSYSTEMS INC 摘要:A method is provided for the semi-synthesis of taxane intermediates useful in the preparation of paclitaxel and docetaxel from 9-dihydro-13-acetylbaccatin III. The preparation of a suitably protected baccatin III backbone from 9-dihydro-13-acetylbaccatin III, and the insertion of the phenylisoserine side chain onto the protected baccatin III from 9-dihydro-13-acetylbaccatin III to form the taxane derivatives, paclitaxel and docetaxel is disclosed.
专利号:US-7098354-B2 优先权日:2002-10-25 标 题:Racemoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indeyl)zirconium compounds 发明人:DAMRAU HANS-ROBERT; MUELLER PATRIK; GARCIA VALERIE; SIDOT CHRISTIAN; TELLIER CHRISTIAN; LELONG JEAN-FRANCOIS 权利人:BASELL POLYOLEFINE GMBH 摘要:The present invention relates to a specific process for the diastereoselective synthesis of rac-diorganosilylbis(2-methylbenzo[e]indenyl)zirconium compounds of the formula I, n nby reacting the silyl-bridged bisindenyl ligand with a dihalozirconium bis(3,5-di-tert-butylphenoxide)-base adduct to form the diorganosilylbis(2-methylbenzo[e]indenyl)zirconium bis(3,5-di-tert-butylphenoxide) and subsequently replacing the phenoxide groups by X using suitable replacement reagents to give the compound of the formula I; where the substituents X can be identical or different and are each F, Cl, Br, I or linear, cyclic or branched C 1-10 -alkyl; and the substituents R can be identical or different and are each linear, cyclic or branched C 1-10 -alkyl or C 6-10 -aryl; and also to the use of these compounds as catalysts.
专利号:US-6608196-B2 优先权日:2001-05-03 标题 :Process for solid supported synthesis of pyruvate-derived compounds 发明人:WANG BING; JANAGANI SATYANARAYANA; CALLAWAY WYETH B; SESSLER JONATHAN L 权利人:GALILEO PHARMACEUTICALS INC 摘要:Provided are processes for synthesizing structurally diverse pyruvate-derived compounds using a parallel approach on a solid phase support. Examples of such a solid phase support include resins which have also been used in solid phase peptide synthesis.
专利号:US-9136483-B1 优先权日:2014-04-17 标 题:Thiophene fused azacoronenes: regioselective synthesis, self organization, charge transport, and its incorporation in conjugated polymers 发明人:LIU YI; HE BO 权利人:LIU YI; HE BO; UNIV CALIFORNIA 摘要:A regioselective synthesis of an azacoronene fused with two peripheral thiophene groups has been realized through a concise synthetic route. The resulting thienoazacoronene (TAC) derivatives show high degree of self-organization in solution, in single crystals, in the bulk, and in spuncast thin films. Spuncast thin film field-effect transistors of the TACs exhibited mobilities up to 0.028 cm 2 V −1 S −1 , which is among the top field effect mobilities for solution processed discotic materials. Organic photovoltaic devices using TAC-containing conjugated polymers as the donor material exhibited a high open-circuit voltage of 0.89 V, which was ascribable to TAC's low-lying highest occupied molecular orbital energy level.
专利号:US-3708477-A 优先权日:1968-06-27 标 题:Process of total synthesis of cephalosporin derivatives and intermediates 发明人:MARTEL J; HEYMES R 权利人:ROUSSEL UCLAF 摘要:PROCESS FOR THE PREPARATION OF RACEMIC OR OPTICALLYACTIVE CEPHALOSPORINE DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-NH2-2-CEPHEM WHEREIN R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, SUBSTITUTED AKYL, ARYL AND SUBSTITUTED ARYL, WHICH COMPRISES THE STEPS OF REACTING AN AMINO ACID OF THE FORMULA R1-NH-CH2-CH2-COOH WITH BENZYL ALCOHOL, CONDENSING THE BENZYL ESTER THUS OBTAINED WITH AN OXALATE, CONVERTING THE BENZYL ESTER OF 2,3DIOXI-4-CARBOXY-PYRROLIDINE INTO THE CORRESPONDING ACID, SUBJECTING SAID ACID TO AMINOMETHYLATION, THUS YIELDING A COMPOUND OF THE FORMULA 1-R1,3-OH,4-(R'-N(-R'')-CH2-)PYRROL-3-IN-2-ONE CONVERTING SAID COMPOUND INTO THE CORRESPONDING 4-ACYLTHIOMETHYL DERIVATIVE, CONVERTING SAID DERIVATIVE INTO THE CORRESPONDING 4-THIOMETHYL DERIVATIVE, CONDENSING SAID DERIVATIVE WITH AN ENAMINE OF THE FORMULA R-OOC-C(-Y)=CH-NH2 TO OBTAIN A THIAZINE DERIVATIVE OF THE FORMULA 2-(Y-CH(-COO-R)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-D)-1,3-THIAZIN-4-ONE CONVERTING SAID THIAZINE DERIVATIVE INTO A COMPOUND OF THE FORMULA 2-(H2N-CH(-COOH)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-)-1,3-THIAZIN-4-ONE SUBJECTING SAID COMPOUND TO THE ACTION OF A TRITYLATION AGENT, RECOVERING THE THREO ISOMER OF THE TRITYLATED DERIVATIVE, LACTAMIZING SAID THREO ISOMER TO OBTAIN THE Y-LACTAM OF DL-6H,7H-CIS-7-TRITYLAMINO-3-AMINOALKYL-CEPH 3-EME-4-CARBOXYLIC ACID, DETRITYLATING SAID Y-LACTAM AND RECOVERING SAID RACEMIC OF OPTICALLY ACTIVE CEPHALOSPORIN DERIVATIVES. THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF THE CORRESPONDING 7ACYLAMINO DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-(R2-NH-)-2-CEPHEM WHEREIN R1 HAS THE ABOVE DEFINITION AND R2 IS THE ACYL OF AN ORGANIC CARBOXYLIC ACID WHICH COMPOUNDS ARE ALSO PART OF THE INVENTION AND ARE USEFUL AS ANTIBIOTICS.