专利号:US-5075450-A 优先权日:1990-06-28 标 题 :Intermediates in the synthesis of 17β-acyl-3-carboxy-androsta-3,5-dienes 发明人:RASMUSSON GARY H; TOLMAN RICHARD L; PATEL GOOL F 权利人:MERCK & CO INC 摘要:New intermediates in the synthesis of 17β-acyl-3-carboxy-androsta-3,5-dienes, of the formula: ##STR1## wherein R 2 is 2-thiopyridyl, and n R 3 is C 2 -C 4 alkoxycarbonyl, C 1 -C 4 , or trifluoromethylsulfonyloxy. The above compounds are useful intermediates in producing testosterone 5α-reductase inhibitors which are useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
专利号:US-11584773-B2 优先权日:2014-04-30 标 题:Phosphorous protecting groups and methods of preparation and use thereof 发明人:DELLINGER DOUGLAS J; MONFREGOLA LUCA; CARUTHERS MARVIN; ROY MITHUN 权利人:AGILENT TECHNOLOGIES INC 摘要:Aspects of the present disclosure include compositions that make use of phosphorus and/or nucleobase protecting groups which find use in the synthesis of long polynucleotides. Phosphorus protecting groups are provided that help increase the stepwise coupling yield and/or phosphorous protecting groups that can be removed during the oxidation step. Amidine nucleobase protecting groups are provided that find use in the subject compositions and methods which provides for e.g., increased resistance to depurination during polynucleotide synthesis. In some instances, the methods and compositions disclosed herein utilize a combination of the phosphorus and amidine nucleobase protecting groups in the synthesis of polynucleotides having a sequence of 200 or more monomeric units in length. Also provided are methods for synthesizing a polynucleotide (e.g., a DNA) using one or more compounds disclosed herein.
专利号:CN-108101741-A 优先权日:2017-12-05 标题 :A method for the tandem synthesis of chiral alcohols by hydration/asymmetric hydrogenation of alkynes
专利号:CN-107522741-A 优先权日:2017-09-04 标题 :A new method for the synthesis of phosphate compounds
专利号:CN-107098829-A 优先权日:2017-06-21 标 题:A method for continuous flow synthesis of α-ketoamides using micro-flow field technology
专利号:CN-107098829-B 优先权日:2017-06-21 标 题 :A method for continuous flow synthesis of α-ketoamides using microfluidic field technology
[参考文献]: S Shaukat Husain, Et Al. P-Trifluoromethyldiazirinyl-Etomidate: A Potent Photoreactive General Anesthetic Derivative Of Etomidate That Is Selective For Ligand-Gated Cationic Ion Channels. J Med Chem. 2010 Sep 9;53(17):6432-44.
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 85. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 175. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 74. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 346. 摘要:Campagne, J. M.; Leclerc, E., Science of Synthesis Knowledge Updates, (2020) 2, 154.