专利号:US-8722886-B1 优先权日:2012-11-13 标题:Methods for the total chemical synthesis of enantiomerically-pure 7-(2′-trimethylsilyl)ethyl camptothecin 发明人:CHEN XINGHAI; HAUSHEER FREDERICK H; MALAKHOV ANDREY; KOCHAT HARRY 权利人:CHEN XINGHAI; HAUSHEER FREDERICK H; MALAKHOV ANDREY; KOCHAT HARRY; BIONUMERIK PHARMACEUTICALS INC 摘要:The present invention discloses and claims five (5) novel, highly efficient synthetic routes for the total synthesis of enantiomerically-pure (i.e., 99%) 7-(2′-trimethylsilyl)ethyl camptothecin (BNP1350; Karenitecin; Cositecan). These aforementioned synthetic schemes are the first to disclose the total syntheses of 7-(2′-trimethylsilyl)ethyl camptothecin using a highly novel direct, non-linear and convergent synthetic strategy which involves annealing the key C7-(trimethylsilyl)ethyl side chain-bearing A ring key synthons to an enantiomerically-pure tricyclic pyridone; rather than through the conventional methodology which incorporates the C7-(trimethylsilyl)ethyl side chain as the final synthetic step on a totally synthesized camptothecin parent compound. The current novel synthetic approaches reported herein since utilize desirably functionalized A-ring with preinstalled trimethyl silyl ethyl side chain, the aforementioned synthetic methodologies have a wider scope of making wide range of pharmaceutically relevant A-ring substituted BNP1350 analogs by substituting desirably functionalized nitro or protected amino phenyl carboxy A-ring as the starting material.
专利号:US-7557099-B2 优先权日:2004-03-01 标题 :Pyrrolobenzodiazepines as key intermediates in the synthesis of dimeric cytotoxic pyrrolobenzodiazepines 发明人:HOWARD PHILIP WILSON; KANG GYOUNG-DONG 权利人:SPIROGEN LTD 摘要:Compounds and a method of synthesis of compounds of formula (Ia) or (Ib): and salts, solvates, and chemically protected forms thereof, wherein the dotted lines indicate the optional presence of a double bond between C1 and C2 or C2 and C3; R 2 and R 3 are independently selected from —H, â•?O, â•?CH 2 , —CN, —R, OR, halo, â•?CH—R, O—SO 2 —R, CO 2 R and COR; R 10 is a carbamate-based nitrogen protecting group; and R 11 is an oxygen protecting group.
专利号:US-10336703-B2 优先权日:2015-05-12 标题 :Process for the synthesis of ivacaftor and related compounds 发明人:REDDY DUMBALA SRINIVASA; NATARAJAN VASUDEVAN; JACHAK GORAKHNATH RAJARAM 权利人:COUNCIL SCIENT IND RES 摘要:The present patent discloses a novel one pot two-step process for the synthesis of ivacaftor and related compounds of [Formula (I)], wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 and Ar 1 are as described above; its tautomers or pharmaceutically acceptable salts thereof starting from indole acetic acid amides.
专利号:US-5077408-A 优先权日:1989-09-20 标 题 :Process for the synthesis of oxazolopyridine compounds 发明人:GUILLAUMET GERALD; FLOUZAT CHRISTINE 权利人:SCIENCE ORGANISATION 摘要:Process for the synthesis of compounds of formula (I): ##STR1## their pyridinium salts and N-oxides, in which formula: the nitrogen of the pyridine ring is situated in the α-, β-, γ- or δ-position with respect to the ring junction; n R 1 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, substituted or unsubstituted amino, phenyl or cyano group; n 0≦m≦2; n R 2 represents a lower alkyl or cycloalkyl group, a 5- or 6-membered heterocycle containing 1 or 2 hetero atoms, substituted or otherwise, or an aryl group ##STR2## such that: R 3 represents a halogen, a substituted or unsubstituted alkyl, a substituted or unsubstituted alkoxy or a nitro, phenyl, substituted or unsubstituted sulfonyl, cyano, thioalkyl, substituted or unsubstituted amino, substituted or unsubstituted sulfinyl, mercapto, hydroxyl or ester group, n 0≦n≦5 n employing trimethylsilyl polyphosphate (PPSE) as a cyclization agent and enabling the compounds of formula (I) to be obtained in virtually quantitative yields. The compounds of formula I have anti-inflammatory, analgesic, and antipyretic activity.
专利号:US-2004092003-A1 优先权日:1997-03-19 标题:Multifunctional ceramic particles as solid supports for solid phase and combinatorial solid phase synthesis 发明人:BOSCHETTI EGISTO; KOCIS PETR 权利人:INVITROGEN CORP 摘要:Inert, thermally and mechanically stable porous ceramic solid phase supports for use in solid phase synthesis of molecules wherein the porous ceramic solid supports can be used under a wide variety of reaction conditions and in synthesis methods, including but not limited to organic, regular, multiple parallel, or combinatorial organic synthesis on a solid phase. Methods of using the porous ceramic solid supports for solid phase synthesis of molecules, for solid phase synthesis of polypeptides or peptidomimetics, for generating combinatorial libraries of linkers, and for combinatorial synthesis of compounds, including small molecules and aromatic and heteroaromatic compounds.
专利号:US-11981648-B2 优先权日:2019-06-13 标题:Method for the synthesis of 3-R-1,4,2-dioxazol-5-ones 发明人:HALL DAVID S; DAHN JEFFERY RAYMOND; HYNES TOREN 权利人:TESLA INC; PANASONIC HOLDINGS CORP 摘要:Provided are methods of preparing 3-R-1,4,2-dioxazol-5-one compounds using convenient and efficient methods. Also provided are 3-R-1,4,2-dioxazol-5-one compounds produced using the methods described.