2-丙烯基锂,Alkaline Earth Salt Of/the/ Methylsulfuric Acid 反应生成 烯丙基雌烯醇 参考文献:De Winter Et Al.,Chemistry And Industry,1959,P. 905 标题:De Winter Et Al.,Chemistry And Industry,1959,P. 905
专利号:WO-2004101594-A1 优先权日:2003-05-14 标题 :New mono-and bismethylene-steroid derivatives and process for their synthesis 发明人:TUBA ZOLTAN; DANCSI LAJOSNE; FRANCSICSNE CZINEGE ERZSEBET; FALKAY GYOERGY; ZUPKO ISTVAN; MARKI ARPAD; MOLNAR CSABA; CSOERGEI JANOS; DUKATNE ABROK VILMA; BALOGH GABOR; MAK MARIANNA 权利人:RICHTER GEDEON VEGYESZET; TUBA ZOLTAN; DANCSI LAJOSNE; FRANCSICSNE CZINEGE ERZSEBET; FALKAY GYOERGY; ZUPKO ISTVAN; MARKI ARPAD; MOLNAR CSABA; CSOERGEI JANOS; DUKATNE ABROK VILMA; BALOGH GABOR; MAK MARIANNA 摘要:The invention relates to new mono- and bismethylene-steroid derivatives of general formula (I) - wherein Z represents two hydrogen atoms or an oxo group; X and Y independently of each other represent either two hydrogen atoms of a CH2= group, with the restriction that at least one of them is CH2= group and if the meaning of Z is oxo group Y represents two hydrogen atoms, R represents a C1-C4 alkyl group, as well as the pharmaceutical compositions containing the above compounds as active ingredients, and the processes for the synthesis of active ingredients and pharmaceutical compositions. The invention also relates to the methods of treatments with these compounds, which means administering to a mammal to be treated with progestogen - including human - effective amount/amounts of the active ingredients of the present invention as such or as medicament. The mono- and bismethylene-steroid derivatives of the general formula (I) have progestogen effect. They can be used as active ingredients of contraceptive medicaments as such or in combination with an estrogen component. Furthermore, they can be used in the treatment of endometriosis and in the substitution therapy of estrogen as gestagen agent beside the estrogen component. The mono- and bismethylene-steroid derivatives of the general formula (I) of the present invention can be synthesized by reacting a compound of the general formula (II), - wherein the meaning of Z, X and Y is as described for the compounds of formula (I) - with an acid anhydride of the general formula (R-CO)2O or with an acid chloride of the general formula R-CO-Cl - wherein R represents a C1-C4 alkyl group - in the presence of a strong acid.
专利号:US-11897827-B1 优先权日:2022-11-22 标 题 :Carbon isotope exchange mediated by vanadium complexes 发明人:BUKHRYAKOV KONSTANTIN 权利人:BUKHRYAKOV KONSTANTIN; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:The subject invention provides catalytical compounds/complexes, compositions comprising such compound/complex, synthesis of the compounds/complexes, and methods of using such compounds/complexes as catalysts in, for example, carbon isotope exchange (CIE) on target bioactive molecules. Methods that allow CIE directly on drug candidates are of great importance to chemistry, biology, and medicine. Especially valuable are catalytic procedures that rely on a limited collection of available labeled materials. The instant method comprises converting a methyl group to terminal â•?CH2 utilizing transfer dehydrogenation catalysts to enable V-based olefin metathesis, followed by a hydrogenation step. The one-pot strategy allows the formal methylation/demethylation sequence and can be applied to an assortment of alkyl-containing compounds.
专利号:US-8017776-B2 优先权日:2003-07-15 标题 :Methods for synthesis of acyloxyalkyl compounds 发明人:BHAT LAXMINARAYAN; GALLOP MARK A 权利人:XENOPORT INC 摘要:Disclosed herein are methods for synthesizing 1-(acyloxy)-alkyl prodrug derivatives of drugs through oxidation of 1-acyl-alkyl derivatives of drugs under anhydrous reaction conditions. The methods typically proceed stereospecifically, in high yield, do not require the use of activated intermediates and/or toxic compounds and are readily amenable to scale-up.
专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-8143437-B2 优先权日:2002-02-19 标题:Methods for synthesis of prodrugs from 1-acyl-alkyl derivatives and compositions thereof 发明人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X 权利人:GALLOP MARK A; XIANG JIA-NING; YAO FENMEI; BHAT LAXMINARAYAN; ZHOU CINDY X; XENOPORT INC 摘要:The present invention provides a method for synthesizing 1-(acyloxy)-alkyl derivatives from 1-acyl-alkyl derivatives, which typically proceeds stereospecifically, in high yield, does not require the use of activated intermediates and/or toxic compounds and is readily amendable to scale-up. The current invention also provides 1-acyl-alkyl derivatives of known drug components and methods for synthesizing these 1-acyl-alkyl derivatives.
专利号:US-12054512-B2 优先权日:2017-11-10 标 题 :Sting modulator compounds, and methods of making and using 发明人:VYSKOCIL STEPAN; CIAVARRI JEFFREY; CULLIS COURTNEY; ENGLAND DYLAN BRADLEY; GOULD ALEXANDRA E; GREENSPAN PAUL; HU YONGBO; LANGSTON STEVEN; LI GANG; MIZUTANI HIROTAKE; OKANIWA MASANORI 权利人:TAKEDA PHARMACEUTICALS CO 摘要:The present disclosure provides STING modulators/agonists, and methods of synthesis and methods for using for the prophylaxis or treatment of cancer and other STING-related diseases.The present disclosure relates to a compound represented by the Formula (I):wherein each symbol is as defined in the description, or a pharmaceutically acceptable salt thereof.
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合成参考文献
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