专利号:US-2023312617-A1 优先权日:2020-07-25 标题 :Process for synthesis of organosilicon compounds from halosilanes 发明人:DOLAI SUKANTA; BHAT SHREEDHAR; TARAFDAR GOURAV 权利人:MOMENTIVE PERFORMANCE MAT INC 摘要:A process for synthesis of an organosilicon compound is provided herein. Also, novel organosilicon compounds prepared by the present process is provided herein. The process comprises the reaction of a halosilane with an organofunctional alkyl halide in the presence of a metal catalyst, a promoter, and an optional co-catalyst. The process provides an efficient synthetic route to produce organosilicon compounds. The process also allows synthesis of organosilicon compounds with a plurality of different functional groups.
专利号:US-7759520-B2 优先权日:1996-11-27 标 题 :Synthesis of selective androgen receptor modulators 发明人:DALTON JAMES T; MILLER DUANE D; YIN DONGHUA; HE YALI 权利人:UNIV TENNESSEE RES FOUNDATION 摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
专利号:US-6995284-B2 优先权日:2000-08-24 标题 :Synthesis of selective androgen receptor modulators 发明人:DALTON JAMES T; MILLER DUANE D; HE YALI; YIN DONGHUA 权利人:UNIV TENNESSEE RES FOUNDATION 摘要:The present invention relates to a synthetic process for the preparation of a novel class of androgen receptor targeting agents (ARTA) which demonstrate androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. The agents define a new subclass of compounds which are selective androgen receptor modulators (SARM) which are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of chronic muscular wasting; e) decreasing the incidence of, halting or causing a regression of prostate cancer; f) oral androgen relacement and/or other clinical therpauetic and/or diagnostic areas. The process of the present invention is suitable for large-scale preparation, since all of the steps give rise to highly pure compounds, thus avoiding complicated purification procedures which ultimately lower the yield. Thus the present invention provides methods for the synthesis of non-steroidal agonist compounds, that can be used for industrial large-scale synthesis, and that provide highly pure products in high yield.
专利号:US-6337393-B1 优先权日:1997-11-13 标 题:Method and composition for chemical synthesis on an open environment support surface using high boiling point organic solvents to control evaporation 发明人:BRENNAN THOMAS M; FRAUENDORF ALBRECHT W 权利人:PROTOGENE LAB INC 摘要:A method for reducing evaporation of a liquid reagent solution during solid phase, micro-scale chemical synthesis of a molecule comprising sub-units on an open environment solid support surface. The method includes the steps of providing an open solid support surface including at least one binding site which is functionalized with a reactive chemical moiety; and depositing a substantially controlled and minute volume of liquid reagent solution onto the support surface, and in contact with the binding site. The reagent solution includes reactants contained in at least one relatively high boiling point solvent, in contrast to standard organic solvents for such reagents. Application of a high boiling point solvent substantially reduces evaporation of the reagent solution in the open environment during synthesis on the solid support while enabling the maintenance of a substantially high reaction yield.
专利号:US-3950389-A 优先权日:1968-10-04 标 题 :Stereospecific total steroidal synthesis via substituted C/D-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##SPC1## n Wherein m is an integer having a value of 1 or 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxymethylene CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl n And reacting them in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##EQU1## wherein R.sub. 6 is selected from the group CONSISTING OF ##EQU2## and LOWER ALKYL; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylene-dioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonyl-methylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
专利号:US-4077983-A 优先权日:1974-06-24 标 题:Stereospecific total steroidal synthesis via substituted C/D-trans indanones 发明人:HAJOS ZOLTAN GEORGE 权利人:HOFFMANN LA ROCHE 摘要:Total synthesis of known progestationally active steroidal materials. The steroids can be synthesized depending on the particular starting reactants selected by employing as intermediates bicyclic compounds of the formula ##STR1## wherein m is an integer having a value of 1 or 2; R 4 is hydrogen or lower alkyl; Z is lower alkylenedioxy, CH(OR 2 ) and carbonyl; R 8 when taken alone is hydrogen; R 9 when taken alone is lower alkoxycarbonyl, aryloxy-carbonyl, lower cycloalkyloxycarbonyl, carbonyl-halide, hydrogen, carboxy, formyl and methylene-X, where X is a leaving group and when taken together are methylene; with the proviso that when Z is carbonyl R 8 when taken alone is hydrogen; R 9 when taken alone is carbonyl halide, hydrogen, carboxy, formyl and methylene-X where X is a leaving group and when taken together are methylene and R 2 is hydrogen, lower alkyl, lower alkoxy-lower alkyl, phenyl-lower alkyl, tetrahydropyranyl, lower alkanoyl, benzoyl, nitrobenzoyl, carboxy-lower alkanoyl, carboxybenzoyl, trifluoroacetyl and camphorsulfonyl n And reacting then in the case where R 8 and R 9 taken together are methylene or R 8 is hydrogen and R 9 is methylene-X with β-keto esters and other analogs of the formula ##STR2## wherein R 6 is selected from the group consisting of ##STR3## lower alkyl; R 7 is lower alkyl; R 15 is selected from the group consisting of oxo, lower alkylenedioxy or (hydrogen and lower alkoxy); B is selected from the group consisting of lower alkoxy-carbonylmethylene, lower-aryloxy-carbonyl-methylene, cyanomethylene, lower alkyl sulfinyl-methylene, lower alkyl sulfonyl-methylene, and R 25 and R 26 are independently selected from the group consisting of hydrogen, hydroxyl and lower alkyl.
1: van Dijk AJ, Duchateau R, Hensen EJ, Meuldijk J, Koning CE. Polyamide synthesis from 6-aminocapronitrile, part 2: heterogeneously catalyzed nitrile hydrolysis with consecutive amine amidation. Chemistry. 2007;13(27):7673-81. doi: 10.1002/chem.200601898. 59(Pt 2):248-53. doi: 10.1099/ijs.0.002204-0.
合成参考文献
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