专利号:US-11773118-B2 优先权日:2019-02-21 标 题:Methods of making high enantioselective secondary alcohols 发明人:YU CHENG-DER TONY; HSIEH YIH-HUANG; LIN SHU-YI; CHAO CHIN-SHENG; HSIEH YIN-CHENG; LAI MING-TAIN 权利人:OBI PHARMA INC 摘要:A new process to synthesis of compound OBI-3424 R-form and S-form products is provided. The “R-formâ€? compound OBI-3423 was first synthesized with 48% overall yield from compound OBI-3424-5 by installation of the labile phosphate motif at later stage. The stereo chemistry is established by 5 steps chemo-enzyme combination synthesis to afford 99% optical purity. After then, the “S-formâ€? compound OBI-3424 is prepared with improving overall yield of 54% from compound OBI-3424-5. The stereo chemistry is established by 4 steps combination of chemo-enzyme synthesis with excellent optical purity of 99%.
专利号:US-7968734-B2 优先权日:2004-07-01 标 题 :Organocatalysts and methods of use in chemical synthesis 发明人:WANG WEI; WANG JIAN; LI HAO 权利人:STC UNM 摘要:The present invention pertains generally to compositions comprising organocatalysts that facilitate stereo-selective reactions and the method of their synthesis and use. Particularly, the invention relates to metal-free organocatalysts for facilitation of stereo-selective reactions, and the method of their synthesis and use.
专利号:US-10458995-B2 优先权日:2016-03-25 标 题 :Combinatorial synthesis and biomarker development 发明人:MOOLA MURALIDHAR REDDY 权利人:MOOLA MURALIDHAR REDDY 摘要:Provided herein are methods, kits, and compositions for use in the diagnosis and treatment of diseases. Peptoids recognized by Alzheimers disease specific antibodies are identified.
专利号:US-9505799-B2 优先权日:2011-05-13 标题:18F-labeled precursor of PET radioactive medical supplies, and preparation method thereof 发明人:CHI DAE-YOON; LEE BYOUNG-SE; PARK CHANSOO; LEE MIN-HYUNG; CHA HYOJIN; CHO WOOJIN; KANG HEEWON; KIM KYUNGHUN 权利人:CHI DAE-YOON; LEE BYOUNG-SE; PARK CHANSOO; LEE MIN-HYUNG; CHA HYOJIN; CHO WOOJIN; KANG HEEWON; KIM KYUNGHUN; FUTURECHEM CO LTD 摘要:The present invention relates to a precursor of positron emission tomography (PET) radioactive medical supplies, a preparation method thereof, and an application thereof, and more specifically, to a precursor having a tetravalent organic salt leaving group, a preparation method, and a method for preparing desired PET radioactive medical supplies in a high radiochemical yield within a short preparation time by introducing 18 F using the same through a single step. The precursor having a tetravalent organic salt leaving group of the present invention can simplify the known complex multistep preparation of radioactive medical supplies into a single step, can save production costs because an excessive amount of a phase transfer catalyst is not required, facilitates separation of a compound after reaction, and enables rapid reaction velocity. The features are appropriate for the mass production of PET radioactive medical supplies by an automated synthesis system.
专利号:US-11739062-B2 优先权日:2017-08-18 标题:Methods for 1,4-diazo N-heterocycle synthesis 发明人:DAI MINGJI; Ye Zhishi 权利人:PURDUE RESEARCH FOUNDATION 摘要:The present disclosure relates to novel synthetic method of making 1, 4-diazo N-heterocycles via intermolecular amphoteric diamination of allenes, and to the compounds made by the novel synthetic method.
专利号:US-8466157-B2 优先权日:2009-03-06 标题:Proteasome inhibitors having chymotrypsin-like activity 发明人:LAWRENCE HARSHANI; GE YIYU; SEBTI SAID M; GUIDA WAYNE 权利人:LAWRENCE HARSHANI; GE YIYU; SEBTI SAID M; GUIDA WAYNE; UNIV SOUTH FLORIDA; H LEE MOFFITT CANCER CT & RES 摘要:Disclosed herein is the use of HLM-008182, as well as its analogues formed via in-house synthesis, as a potent proteasome inhibitors. A new method was developed for HLM-008182 through a four-step protocol and the method was further optimized to a two step protocol. The synthesis in both protocols was regioselective with TiCl 4 . The reaction was highly efficient with microwave assisted heating and THF as solvent. The modification around the molecule HLM-008182 established primary SAR, indicating that the proteasome inhibition activity was a function of the 2-side chain.