3,4-二氯碘苯置于盐酸,氯磺酸体系中,用 二氯甲烷 用作溶剂,化学反应 23.5H,反应生成4-(3,4-二氯苯)-3,4-二氢-2H-萘-1-酮 参考文献:A Catalytic Enantioselective Synthetic Route To The Important Antidepressant Sertraline 标题:A Catalytic Enantioselective Synthetic Route To The Important Antidepressant Sertraline 摘要:An Efficient Catalytic Enantioselective Synthesis Of The Important Antidepressant Sertraline Is Described (Scheme I). Doi:10.1016/s0040-4039(00)73503-9
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: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).
专利号:WO-0130742-A1 优先权日:1998-11-23 标题:Improved synthesis of racemic sertraline
专利号:US-5750794-A 优先权日:1993-11-30 标 题:Process for preparing chiral tetralone 发明人:QUALLICH GEORGE J 权利人:PFIZER 摘要:A process for preparing the chiral (4S)-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone is disclosed wherein racemic 4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenone is asymmetrically reduced by contacting the racemic tetralone with an asymmetric reagent to produce a mixture of cis and trans alcohols, separating the cis from the trans alcohols, and oxidizing the (4S) enantiomer of the resulting cis and trans alcohols. Also disclosed are novel intermediates used in the synthesis of the above chiral tetralone.
参考标题:Synthesis Of 4(S)-(3,4-Dichlorophenyl)-3,4-Dihydro-1(2H)-Naphthalenone By Sn2 Cuprate Displacement Of An Activated Chiral Benzylic Alcohol 作者:George J. Quallich,Teresa M. Woodall |发布日期:1992.11 摘要:Two Routes For The Preparation Of 4(S)-(3,4-Dichlorophenyl)-3,4-Dihydro-1(2H)-Naphthalenone Are Reported. The Most Efficient Route Generates A Chiral Benzylic Alcohol By Catalytic Asymmetric Oxazaborolidine Reduction Of A γ-Ketoester That Is Subsequently Activated And Displaced In An Sn2 Manner With A Higher Order Cuprate. Intramolecular Friedel-Crafts Cyclization Of The Resulting T-Butylester Affords
合成参考文献
摘要:S109 | PARCEDC | List of 7074 potential endocrine disrupting compounds (EDCs) by PARC T4.2 | DOI:10.5281/zenodo.10944198