专利号:US-10995049-B2 优先权日:2019-07-19 标 题 :Total synthesis of prostaglandin J natural products and their intermediates 发明人:LI JIAMING; XU CHEN; AHMED TONIA S; GRUBBS ROBERT H; STOLTZ BRIAN M 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure is directed to methods of preparing prostaglandin J natural products by stereoretentive metatheses reactions and intermediates used in the synthesis of these natural products, including the use of intermediates of Formula (I-A), where R 1 is defined in the specification
专利号:US-11891375-B2 优先权日:2021-07-26 标 题 :Method for the synthesis of 2,4-dimethylpyrimidin-5-ol, intermediates, and method for the synthesis of Lemborexant using the intermediates 发明人:AKHATOU ABDESLAM; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:A method is for the synthesis of 2,4-dimethylpyrimidin-5-ol, which can be used as an intermediate compound in the synthesis of Lemborexant. The method includes reacting a nitrophenyl compound with N,N-dimethylformamide diethyl acetal.
专利号:US-9388131-B2 优先权日:2011-04-27 标题:Automated synthesis of small molecules using chiral, non-racemic boronates 发明人:BURKE MARTIN D; LI JUNQI; GILLIS ERIC P 权利人:UNIV ILLINOIS 摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
专利号:US-11479577-B2 优先权日:2016-05-18 标题:Intermediates for the synthesis of bile acid derivatives, in particular of obeticholic acid 发明人:WEYMOUTH-WILSON ALEXANDER; KOMSTA ZOFIA; WALLIS LAURA; EVANS TIMOTHY; DAVIES IEUAN; OTTER CARL; BATCHELOR RHYS 权利人:NZP UK LTD 摘要:The present invention relates to compounds which are intermediates in the synthesis of bile acid derivatives with pharmacological activity. The invention relates to compounds of general formula (I):wherein:, R1, R2, R3, R4, R5, R6 and Y are as defined herein.The compounds are intermediates in the synthesis of synthetic bile acids which are useful in the treatment of conditions such as liver disease. In addition, the invention relates to a method of synthesizing these intermediates and a method of preparing obeticholic acid and obeticholic acid analogues from the compounds of the invention.
专利号:US-7247287-B2 优先权日:2003-06-11 标 题 :Synthesis of aluminophosphates and silicoaluminophosphates 发明人:CAO GUANG; SHAH MATU J 权利人:EXXONMOBIL CHEM PATENTS INC 摘要:The invention is directed to a method of synthesising silicoaluminophosphate and aluminophosphate molecular sieves using synthesis templates that contain at least one template of general formula R 1 R 2 N—R 3 , wherein R 1 and R 2 are independently selected from the group consisting of alkyl groups having from 1 to 3 carbon atoms and hydroxyalkyl groups having from 1 to 3 carbon atoms; R 3 is selected from the group consisting of 4- to 8-membered cycloalkyl groups, optionally substituted by 1 to 3 alkyl groups having from 1 to 3 carbon atoms, and 4- to 8-membered heterocyclic groups having from 1 to 3 heteroatoms, said heterocyclic groups being optionally substituted by 1 to 3 alkyl groups having from 1 to 3 carbon atoms and the heteroatoms in said heterocyclic groups being selected from the group consisting of O, N, and S. In particular, the present invention relates to the synthesis of silicoaluminophosphate molecular sieves of the CHA framework type having a low silicon to aluminium atomic ratio.
专利号:US-6184168-B1 优先权日:1997-09-22 标题:Synthesis of 1,4-trans-polybutadiene using a lanthanide organic acid salt catalyst 发明人:LYNCH THOMAS J 权利人:BRIDGESTONE CORP 摘要:The invention provides a catalyst composition, comprising: (a) an organolithium compound; and, (b) an organic acid salt of lanthanide series element; wherein: (1) only components (a) and (b) are required to promote the synthesis of 1,4-trans-polybutadiene; (2) the ratio of component (a) to component (b) is selected to maximize formation of the trans structure of said 1,4-trans-polybutadiene; and, (3) components (a) and (b) are selected for enabling further diblock synthesis. The invention further contemplates a process for using the catalyst to synthesize 1,4-trans-polybutadiene and other polymers and copolymers having trans configuration in the conjugated diene monomer contributed units.
参考文献:10.1016/j.bmc.2011.06.069 摘要:Zhang L, Feng L, Jia Q, Xu J, Wang R, Wang Z, Wu Y, Li Y. Effects of β-glucosidase hydrolyzed products of harpagide and harpagoside on cyclooxygenase-2 (COX-2) in vitro. Bioorg Med Chem. 2011 Aug 15;19(16):4882–6. doi: 10.1016/j.bmc.2011.06.069.