专利号:WO-0140193-A1 优先权日:1999-12-03 标题:Method for the synthesis of pyrazolines 发明人:BOLDI ARMEN M 权利人:CHEMRX ADVANCED TECHNOLOGIES I; BOLDI ARMEN M 摘要:The present invention provides a method for the synthesis of compounds of Formula (I). Also claimed are novel intermediates and their methods of synthesis.
专利号:US-6022963-A 优先权日:1995-12-15 标 题:Synthesis of oligonucleotide arrays using photocleavable protecting groups 发明人:MCGALL GLENN H; NAM NGO QUOC 权利人:AFFYMETRIX INC 摘要:Novel compounds are provided which are useful as linking groups in chemical synthesis, preferably in the solid phase synthesis of oligonucleotides and polypeptides. These compounds are generally photolabile and comprise protecting groups which can be removed by photolysis to unmask a reactive group. The protecting group has the general formula Ar-C(R1)(R2)-O-C(O)- wherein: Ar is an optionally substituted fused polycyclic aryl or heteroaromatic group or a vinylogous derivative thereof; R1 and R2 are independently H, optionally substituted alkyl, alkenyl or alkynyl, optionally substituted aryl or optionally substituted heteroaromatic, or a vinylogous derivative of the foregoing; and X is a leaving group, a chemical fragment linked to Ar-C(R1)(R2)-O-C(O)- via a heteroatom, or a solid support; provided that when Ar is 1-pyrenyl and R1=R2=H, X is not linked to Ar-C(R1)(R2)-O-C(O)- via a nitrogen atom. Preferred embodiments are those in which Ar is a fused polycyclic aromatic hydrocarbon and in which the substituents on Ar, R1 and R2 are electron donating groups. A particularly preferred protecting group is the 'PYMOC' protecting group, pyrenylmethyloxycarbonyl, where Ar=pyrenyl and R1=R2=H. Also provided is a method of forming, from component molecules, a plurality of compounds on a support, each compound occupying a separate predefined region of the support, using the protected compounds described above.
专利号:US-7173059-B2 优先权日:2003-05-08 标题:Intermediates useful in the synthesis of HIV-protease inhibitors and methods for preparing the same 发明人:ALBIZATI KIM FRANCIS; BABU SRINIVASAN 权利人:AGOURON PHARMA 摘要:Optically active 3-amino-butene and 1,2-dihydroxy-3-amino-butane intermediate compounds, useful in the synthesis of HIV-protease inhibitors and methods of preparing these intermediate compounds are disclosed.
专利号:US-6472534-B2 优先权日:1999-10-21 标 题:Methods for the preparation of intermediates in the synthesis of HIV-protease inhibitors 发明人:BORER BENNETT C; ZOOK SCOTT E; BUSSE JULIETTE K 权利人:AGOURON PHARMA 摘要:Methods for the preparation of chemical intermediates in the synthesis of HIV-protease inhibitors related to and including nelfinavir mesylate are disclosed. The method of this invention comprises converting tetrohydran derivatives into oxazolines to provide key reaction intermediates for the preparation of nelfinavir. Also disclosed is a method for the preparation of a chiral amino alcohol from an epoxy-tetrahydrofuran.
专利号:US-2024425446-A1 优先权日:2023-06-23 标题:Dichloromethane-free synthesis of cyclopropenimines 发明人:HEDRICK JAMES L; CAMPOS LUIS M; PARK NATHANIEL H; WU DINO 权利人:IBM; THE TRUSTEE OF COLUMBIA UNIV IN THE CITY OF NEW YORK 摘要:A process of forming a cyclopropenimine (CPI) is disclosed. The process includes obtaining a solution of pentachlorocyclopropane (PCC) dissolved in a first solvent and adding a secondary amine to the solution. The process further includes obtaining precipitated products, including a CPI chloride (CPI−Cl) salt and a secondary amine salt, of a reaction between the secondary amine and the PCC and mixing the precipitated products in a second solvent. The CPI−Cl salt is substantially soluble in the second solvent and the secondary amine salt is substantially insoluble in the second solvent. A CPI composition, an apparatus containing the CPI composition, a process of capturing carbon dioxide (CO2) with the CPI composition, and a process of generating carbonate with the CPI composition are also disclosed.
专利号:US-7855285-B2 优先权日:2005-06-14 标 题:Methods for selective N-9 glycosylation of purines 发明人:ROBINS MORRIS J; ZHONG MINGHONG 权利人:UNIV BRIGHAM YOUNG 摘要:A process for providing regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs is described. The introduction of the sugar moiety on to 6-(azolyl)-substituted purine bases is performed so that highly stereoselective formation of the β anomers of only the 9 position regioisomers of the purine nucleoside analogs (either D or L enantiomers) is obtained. This regiospecific and stereoselective introduction of the sugar moiety allows the synthesis of nucleoside analogs, and in particular 2′-deoxy, 3′-deoxy, 2′-deoxy-2′-halo-arabino and 2′,3′-dideoxy-2′-halo-threo purine nucleoside analogs, in high yields without formation of the 7-positional regioisomers. Processes for providing novel 6-(azolyl)purines for the regiospecific and highly stereoselective synthesis of 9-β anomeric purine nucleoside analogs are described. The compounds are drugs or intermediates to drugs.