专利号:US-7465842-B2 优先权日:2004-08-26 标 题 :Enantioselective biotransformation for preparation of protein tyrosine kinase inhibitor intermediates 发明人:KUNG PEI-PEI; MARTINEZ CARLOS; TAO JUNHUA 权利人:AGOURON PHARMA 摘要:The invention relates to biocatalytic methods for preparing enantiomerically pure stereoisomers of 1-(2,6-dichloro-3-fluorophenyl)ethanol. Disclosed are methods of preparation of the desired (S)-enantiomer, which methods are based on a combination of enzymatic resolution, chemical esterification and chemical hydrolysis with inversion of 1-(2,6-dichloro-3-fluorophenyl)ethyl esters or stereoselective bio-reduction of 2,6-dichloro-3-fluoro-acetophenone with a biocatalyst such as an enzyme or a microorganism. The chiral (S)-enantiomer can be used in the synthesis of certain enantiomerically enriched, ether linked 2-aminopyridine compounds that potently inhibit auto-phosphorylation of human heptocyte growth factor receptor.
专利号:US-9919064-B2 优先权日:2012-08-10 标 题 :Compositions, methods, and systems for the synthesis and use of imaging agents 发明人:CESATI RICHARD R; RADEKE HEIKE S; PANDEY SURESH K; PUROHIT AJAY; ROBINSON SIMON P 权利人:LANTHEUS MEDICAL IMAGING INC 摘要:The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.
专利号:US-11401277-B2 优先权日:2017-11-29 标 题 :Anti-bacterial heterocyclic compounds and their synthesis 发明人:PEER MOHAMED SHAHUL HAMEED; BHARATHAM NAGAKUMAR; KATAGIHALLIMATH NAINESH; SHARMA SREEVALLI; NANDISHAIAH RADHA; RAMACHANDRAN VASANTHI 权利人:BUGWORKS RES INC 摘要:The invention relates to compounds of Formula I and Formula (B) along with their stereoisomers, pharmaceutically acceptable salts, complexes, hydrates, solvates, tautomers, polymorphs, racemic mixtures, optically active forms, and pharmaceutically active derivatives thereof. These compounds are useful for killing or inhibiting the growth of a microorganism selected from the group consisting of bacteria, virus, fungi, and protozoa.
专利号:US-11229713-B2 优先权日:2014-11-25 标题:Methods and compositions for 18F-radiolabeling of biologics 发明人:DONNELLY DAVID 权利人:BRISTOL MYERS SQUIBB CO 摘要:The invention relates to water soluble 18 F-prosthetic groups and the synthesis and use of 18 F-labeled biological molecules containing the 18 F-prosthetic groups for imaging various processes within the body, for detecting the location of molecules associated with disease pathology, and for monitoring disease progression are disclosed.
专利号:CN-112125841-A 优先权日:2020-10-23 标题:A new method for the synthesis of crizotinib intermediates
专利号:US-4552967-A 优先权日:1984-01-12 标 题:Process for the synthesis of intermediates in the preparation of diaminopyridines 发明人:GREENE JAMES M; LAVAGNINO EDWARD R; PIKE ANDREW J; TAYLOR EDWARD C 权利人:LILLY CO ELI 摘要:The present invention relates to a process for preparing aminonitropyridines comprising reacting an alkoxynitropyridine with ammonium acetate.
[参考文献]: S L Gwaltney Nd, Et Al. Novel Sulfonate Derivatives: Potent Antimitotic Agents. Bioorg Med Chem Lett. 2001 Jul 9;11(13):1671-3.
合成参考文献
摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#04089 摘要:Kleemann, A.; Engel, J.; Kutscher, B.; Reichert, D., Pharmaceutical Substances[Online], Thieme: Stuttgart, (2014).