专利号:US-10266481-B2 优先权日:2014-06-20 标题:Organocatalytic asymmetric synthesis of antidepressants 发明人:VAITHIYANATHAN VENKATARAMASUBRAMANIAN; KALSHETTI RUPALI GUNDAPPA; ARUMUGAM SUDALAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a short enantioselective synthesis of 1-amino aryl tetraline compounds of Formula 1 via nucleophilic enamine catalysis using organocatalyst such as proline. n n n n n n n n n n n n wherein R 1 and R 2 represent independent of each other hydrogen, (un)substituted or substituted amine; n R 3 and R 4 represent independent of each other hydrogen or halogen.
专利号:EP-3800178-A1 优先权日:2019-10-01 标题:Preparation of enamide intermediate for the synthesis of dasotraline 发明人:BALLETTE ROBERTO; DOBARRO RODRÃ?GUEZ ALICIA 权利人:MOEHS IBERICA SL 摘要:The present invention relates to a process for the preparation of N -(( S )-4-(3,4-dichlorophenyl)-3,4-dihydronaphthalen-1-yl)acetamide, which is a suitable intermediate for the synthesis of dasotraline or a pharmaceutically acceptable salt thereof, as well as to a process for the preparation of dasotraline or a pharmaceutically acceptable salt thereof using said N -(( S )-4-(3,4-dichlorophenyl)-3,4-dihydronaphthalen-1-yl)acetamide intermediate.
专利号:WO-2016088138-A1 优先权日:2014-12-01 标题 :Diphenyloxiranes, process for preparation thereof, and its use in an enantioselective synthesis of (+)-sertraline 发明人:SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM; KAMBLE ROHIT BALKRISHNA 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses substituted diphenyloxiranes and process for synthesis thereof. The present invention also provides a process for production of enantiomerically pure anti-3,3' -diphenylmethyloxirane and anti-3,3'- diphenylpropan- 1,2-diol from racemic anti-3,3' -diphenylmethyloxirane using hydrolytic kinetic resolution. Further it provides a process for preparation of enantioselective (+)- Sertraline from anti-3,3' -diphenylpropan-1,2-diol.
专利号:US-2001044142-A1 优先权日:2000-04-28 标题:Microbial reductase useful for the stereoselective reduction of a racemic tetralone 发明人:BROWN MARIA S; FEDECHKO RONALD W; WONG JOHN W 摘要:The present invention relates to novel compositions of matter comprising an enzyme activity capable of carrying out the following stereoselective reduction of a racemic tetralone: n n n The chiral tetralone can be used in the synthesis of sertraline, well known to be useful, for example, as an antidepressant and anorectic agent, and in the treatment of chemical dependencies, anxiety-related disorders, premature ejaculation, cancer and post-myocardial infarction.
专利号:WO-2020025646-A1 优先权日:2018-07-30 标题:An omega-transaminase enzyme 发明人:MAGUIRE ANITA; GAVIN DECLAN; O'GARA FERGAL; REEN JERRY 权利人:UNIV COLLEGE CORK NATIONAL UNIV OF IRELAND CORK 摘要:An isolated w-transaminase enzyme comprising an amino acid sequence of SEQUENCE ID NO: 1, or encoded by a nucleic acid sequence of SEQUENCE ID NO: 2, is provided which is derived from marine sponge Pseudovibrio sp.. Also provided are functional variants of the w-transaminase enzyme that are isolated, have at least 80% sequence identity with SEQUENCE ID NO: 1, and are capable of enantioselectively resolving a racemic amine by transformation to a ketone by oxidative deamination, or enantioselectively resolving a racemic ketone by transformation to an amine by reductive amination, in which the amine and ketone typically contain a stereocentre removed from the reacting site. An example of a functional variant is SEQUENCE ID NO:3. In one embodiment, the functional variant is capable of enantioselectively transforming a (4S) -tetralone intermediate in the synthesis of sertraline, in which the functional variant displays remote stereospecificity for the tetralone intermediate.
专利号:US-6589777-B1 优先权日:1998-10-29 标题:Stereoselective microbial reduction of a racemic tetralone 发明人:MORSE BROOK K; TRUESDELL SUSAN J; WONG JOHN W 权利人:PFIZER 摘要:The present invention relates to processes for carrying out the following stereoselective microbial reduction of a racemic tetralone: n which comprises: contacting a compound of formula (I) with a microorganism, or an enzyme reduction system capable of accomplishing the subject reduction comprising an enzyme derived from said microorganism and a co-factor for said enzyme, and incubating the resulting mixture under conditions sufficient to yield the (4R) tetralol of formula (II) and to leave substantially unreacted the (4S) tetralone of formula (V) or “chiral tetralone.â€? The chiral tetralone can be used in the synthesis of sertraline. The subject process further optionally comprises the separation of the (4S) tetralone of formula (V) from the (4R) tetralol of formula (II). The (4R) tetralol can be recycled to produce the compound of formula (I) and the subject process repeated to result in even more of the desired (4S) tetralone of formula (V).
参考标题:α,α-Diarylethylene Glycols As Valuable Precursor For Synthesis Of 1,1-Diarylethenes And α,α-Diaryl Acetaldehydes 作者:Praveen Kumar Tiwari,Balasubramaniam Sivaraman,Indrapal Singh Aidhen |发布日期:2017.7.7 摘要:Towards Assembling Of Diarylmethine Unit Present In Biologically Important Molecules, We Have Developed A New Weinreb Amide (Wa) Based Building Block, Derived From Glycolic Acid. The Wa Functionality Present In This Building Block Had Allowed The Sequential Addition Of Various Arylmagnesium Bromide Reagents In A Controlled Manner Enabling Assembling Of Diarylmethine Unit. The Developed Synthetic Route