专利号:US-7118627-B2 优先权日:2003-12-04 标 题 :Synthesis of colloidal PbS nanocrystals with size tunable NIR emission 发明人:HINES MARGARET A; SCHOLES GREGORY D 权利人:HINES MARGARET A; SCHOLES GREGORY D 摘要:The present invention discloses a method for synthesis of narrowly dipsersed colloidal PbS nanocrystals that offer size-tunable near-infrared emission. The stability and processibility of these near-infrared emitting quantum dots makes them ideal materials for device applications. The use of cost-effective and non-pyrophoric precursors as well as the success of larger scale reactions means the present invention provides a method for the industrial scale production of PbS nanocrystals.
专利号:US-2023303546-A1 优先权日:2020-03-05 标题:Process And Intermediates For The Preparation Of Pyroxasulfone 发明人:RECSEI CARL; BARDA YANIV 权利人:ADAMA AGAN LTD 摘要:The invention relates to a process for preparing a key intermediate of Formula (I) in the synthesis of pyroxasulfone. The process comprises reacting an isoxazole of Formula (II) with a thionating reagent to create an S-substituted thioisoxazole of Formula (III); and combining the S-substituted thioisoxazole of Formula (III) with a pyrazole of the Formula (IV) by introducing a methylene bridge, to obtain a compound of Formula (I). The invention also relates to novel S-substituted thioisoxazole of Formula (III) and processes of preparation thereof, wherein L1 is halogen or an anionic residue derived from an acid; R is an organic residue derived from a suitable thionating reagent: dimethyl thioformamide, thiosulfate salts, dithiooxamide, alkyl xanthate salts, thiobenzamide, V-substituted thiourea and thioacetate salts.
专利号:WO-0146142-A1 优先权日:1999-12-20 标题:A process for the regioselective synthesis of 2,2-dialkyl-4-substituted piperidines 发明人:HEATH PERRY CLARK 权利人:LILLY CO ELI; HEATH PERRY CLARK 摘要:The present invention provides a process for preparing a compound of formula (I): wherein R?1 and R2¿ each independently represent C¿1?-C4 alkyl; and X represents an alkyl, alkenyl, cycloalkyl, aryl, substituted aryl, heterocycle, or substituted heterocycle, comprising treating a compound of formula (II): wherein Q represents Cl or Br, with a suitable base followed by addition of a suitable Lewis acid and addition of a compound of formula R?-M+¿ wherein M+ is a suitable cation.
专利号:US-5112972-A 优先权日:1989-06-02 标 题 :Synthesis of chroman derivatives 发明人:GERICKE ROLF; BAUMGARTH MANFRED; LUES INGEBORG; BERGMANN ROLF; PEYER DE 权利人:MERCK PATENT GMBH 摘要:The invention relates to new chroman derivatives of the formula I in which R1 is A, R2 and R8 are each H or A, R1 and R2 together are also alkylene with 3-6 C atoms, R3 is OH, OA or OAc, R4 is H, R3 and R4 together are also a bond, R5 is Ar or CnH2n-R9, R9 is alkenyl or alkynyl with 2-4 C atoms in each case, OH, OA, CHO, CO-A, CS-A, COOH, COOA, COO-alkyl-Ar, CS-OA, NO2, NH2, NHA, NA2, CN, F, Cl, Br, I, CF3, SA, SO-A, SO2-A or Ar, Ar is a phenyl group which is unsubstituted or substituted once or twice by R10, R6, R7 and R10 are each H, A, HO, AO, CHO, ACO, CF3CO, ACS, HOOC, AOOC, AO-CS, ACOO, A-CS-O, hydroxy-alkyl, mercapto-alkyl, NO2, NH2, NHA, NA2, CN, F, Cl, Br, I, CF3, AS, ASO, ASO2, AO-SO, AO-SO2, AcNH, AO-CO-NH, H2NSO, HANSO, A2NSO, H2NSO2, HANSO2, A2NSO2, H2NCO, HANCO, A2NCO, H2NCS, HANCS, A2NCS, ASONH, ASO2NH, AOSONH, AOSO2NH, ACO-alkyl, nitro-alkyl, cyano-alkyl, A-C(=NOH), A-C(=NNH2), H2PO3 or A2PO3, n is 1, 2 or 3, A is alkyl with 1-6 C atoms, -alkyl is alkylene with 1-6 C atoms and AC is alkanoyl with 1-8 C atoms or aroyl with 7-11 C atoms, and the salts thereof which display effects on the cardiovascular system and can be used for the treatment or prophylaxis of heart failure, angina pectoris, high blood pressure, incontinence and alopecia.
专利号:US-7612106-B2 优先权日:2004-12-23 标题 :Fused pyrazole derivatives and methods of treatment of metabolic-related disorders thereof 发明人:BOATMAN P DOUGLAS; SCHRADER THOMAS O; SEMPLE GRAEME; SKINNER PHILIP J; JUNG JAE-KYU 权利人:ARENA PHARM INC 摘要:The present invention relates to certain fused pyrazole derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists for the RUP25 receptor. n nAlso provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of metabolic-related disorders, including dyslipidemia, atherosclerosis, coronary heart disease, insulin resistance, type 2 diabetes, Syndrome-X and the like. In addition, the present invention also provides for the use of the compounds of the invention in combination with other active agents such as those belonging to the class of α-glucosidase inhibitors, aldose reductase inhibitors, biguanides, HMG-CoA reductase inhibitors, squalene synthesis inhibitors, fibrates, LDL catabolism enhancers, angiotensin converting enzyme (ACE) inhibitors, insulin secretion enhancers, DP receptor antagonists, and the like.
专利号:US-6852711-B2 优先权日:1998-09-11 标题:HIV protease inhibitors 发明人:BOYER JR FREDERICK EARL; DOMAGALA JOHN MICHAEL; ELLSWORTH EDMUND LEE; GAJDA CHRISTOPHER ANDREW; HAGEN SUSAN ELIZABETH; LOVDAHL MICHAEL JAMES; LUNNEY ELIZABETH ANN; MARKOSKI LARRY JAMES; PRASAD JOSYULA VENKATA NAGENDR; TAIT BRADLEY DEAN 权利人:AGOURON PHARMA 摘要:The present invention relates to novel dihydropyrones with tethered heterocycles having improved pharmacologic properties which potently inhibit the HIV aspartyl protease blocking HIV infectivity. The dihydropyrones are useful in the development of therapies for the treatment of viral infections and diseases, including AIDS. The present invention is also directed to methods of synthesis of the dihydropyrones and intermediates useful in the preparation of the final compounds.
[参考文献]: Ingmar Persson, Et Al. Coordination Chemistry Study Of Hydrated And Solvated Lead(Ii) Ions In Solution And Solid State. Inorg Chem. 2011 Feb 7;50(3):1058-72. [参考文献]: Kozo Fukumoto, Et Al. Desulfurization Of N,N-Dimethylthioformamide By Hydrosilane With The Help Of An Iron Complex. Isolation And Characterization Of An Iron-Carbene Complex As An Intermediate Of C=double Bond Cleavage. Chem Commun (Camb). 2012 Apr 21;48(32):3809-11.
合成参考文献
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