专利号:WO-2012153162-A1 优先权日:2011-05-12 标题 :Novel method for preparation of atovaquone 发明人:ROY BHAIRAB NATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; TRIVEDI ANURAG 权利人:LUPIN LTD; ROY BHAIRAB NATH; SINGH GIRIJ PAL; LATHI PIYUSH SURESH; AGRAWAL MANOJ KUNJABIHARI; MITRA RANGAN; TRIVEDI ANURAG 摘要:Provided is a process of preparation of 2-[ trans ,-4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy- 1,4-naphthoquinone, i.e. Atovaquone [I] which is cost effective, green, and eco-friendly process, without separation of any diastereomers or geometric isomers of intermediates obtained during the reactions. Also provided is separation of ' cis ' and ' trans ' isomer of intermediates VI, VII and VIII through selective crystallization in an appropriate solvent. A method for converting 2-[ cis ,-4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthoquinone to 2-[ trans -4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-l,4-naphthoquinone in presence of Lewis/ Bronsted acid is also provided. A process for preparation of compound 2-(4-(4- chlorophenyl)- 1 -hydroxy cyclohexyl)-3,4-dihydronaphthalen- 1 (2H)-one [IV] comprising condensation of (1,2-dihydronaphthalen-4-yloxy)trimethylsilane [II] with 4-(4- chlorophenyl)cyclohexanone [III] in presence of Lewis acid in organic solvent. The invention also encompasses a highly efficient and atomeconomic process for synthesis of compound [III] i.e. 4-(4-chlorophenyl)cyclohexanone as well as a process for synthesis of 2-[ cis -4-(4'- chlorophenyl)cyclohexyl]-3-hydroxy-l,4-naphthoquinone. Further provided is a process for isomerization of cis- Atovaquone i.e. 2-[ cis -4-(4'-chlorophenyl)cyclohexyl]-3-hydroxy-l,4- naphthoquinone to tnms-Atovaquone i.e. 2-[ trans -4-(4'-chlorophenyl)cyclohexyl]-3- hydroxy- 1,4-naphthoquinone in presence of Lewis acid.
专利号:US-7544794-B1 优先权日:2005-03-11 标题 :Method for sequencing DNA and RNA by synthesis 发明人:BENNER STEVEN ALBERT 权利人:BENNER STEVEN ALBERT 摘要:This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that are nucleic acid analogs. More specifically, this invention relates to compositions that allow the sequencing of oligonucleotides by synthesis, and processes for sequencing by synthesis that exploit these compositions. Most specifically, the instant invention discloses compositions of matter that are 5′-triphosphates of ribo- and 2′-deoxyribonucleosides wherein the 3′-OH group is replaced by a 3′-ONHR group in the alpha configuration, wherein R is either a H or CH 3 group. Also disclosed are these triphosphates where the nucleobase carries, via a linker, a reporter groups, such as a fluorescent species that can be used in single- or multi-copy DNA sequencing, or a tag that can be visualized by ultramicroscopy. Also disclosed are processes that use these compositions to do sequencing by synthesis.
专利号:CN-102321891-A 优先权日:2011-09-19 标题:A high-yield electrochemical method for the synthesis of 2,2'-dichlorohydroazobenzene
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.
专利号:CN-116874360-A 优先权日:2023-09-06 标 题:A kind of synthesis method of bupavaquone
专利号:CN-116874360-B 优先权日:2023-09-06 标题:A kind of synthesis method of bupavaquone
参考标题:The Vicinal Functionalization Of Olefins: A Facile Route To The Direct Synthesis Of β-Chlorohydrins And β-Chloroethers 作者:Peraka Swamy,Macharla Arun Kumar,Marri Mahender Reddy,Mameda Naresh,Kodumuri Srujana,Nama Narender 摘要:An Efficient And Environmentally Benign Protocol For The Synthesis Of Vicinal Chlorohydroxy And Chloromethoxy Derivatives In A Highly Regioselective Manner From Olefins Using Nh4Cl As A Chlorine Source And Oxone As An Oxidant In Aqueous Acetone And Methanol Is Demonstrated. This Methodology Offers An Additive And Metal Chloride Free Approach And Is Endowed With Simple Reaction Conditions, High Yields
合成参考文献
摘要:Herter, S.; Turner, N. J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 3, 82.