CAS: 16874-17-2; (S)-Tert-Butyl 2-Amino-3-Phenylpropanoate

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📜1-Benzyl-2-Tert-Butoxycarbonyl-3-Phenylaziridine置于10% Pd/c,氢气体系中,用 甲醇 用作溶剂,50.0 °C,101.33 Kpa 条件下,反应 24.0H,以75%的收率获得l-苯基丙氨酸叔丁酯
参考文献:General Entry To Asymmetric One-Pot [n + 2 + N] Cyclization For The Synthesis Of Three-To Seven-Membered Azacycloalkanes
标题:General Entry To Asymmetric One-Pot [n + 2 + N] Cyclization For The Synthesis Of Three-To Seven-Membered Azacycloalkanes
摘要:Enantio-And Diastereoselective One-Pot Synthesis Of Three-To Seven-Membered Cis-Azaheterocycles Was Achieved Using A Triggered Asymmetric Conjugate Addition Reaction Of Lithium Amide With An Enoate,Followed By Alkylation Of The Resulting Lithium Enolate With Alpha,Omega-Dihaloalkane And N-Alkylation. Isomerization Of Cis-Azaheterocycles With A Base Yielded The Trans-Product,Constituting A One-Pot Synthesis Of Cis-Azacycles And A Two-Step Synthesis Of Trans-Azacycles. The Four-Step Asymmetric Synthesis Of Nemonapride Highlights The General Utility Of The Method.
Doi:10.1021/jo301495A

专利信息

专利号:US-4346039-A
优先权日:1981-03-19
标 题 :Synthesis of ochratoxins
发明人：KRAUS GEORGE A
权利人:UNIV IOWA STATE RES FOUND INC
摘要:A simple, direct synthesis route is provided for Ochratoxin compounds, particularly Ochratoxin A, Ochratoxin B, and Ochratoxin C. The reaction involves treating the dimethyl ester of 2-hydroxy-4-methylbenzene-1,3-dioic acid with a deprotonating agent, followed by addition of acetaldehyde, to provide a precursor compound, which can conveniently be converted to Ochratoxins A, B or C. The synthesis route allows for the first time laboratory and industrial scale synthesis of ochratoxins A, B and C in large quantities and pure form making them available as toxins, for use as anti-toxin investigation works, and for biological activity investigations and residue studies.

专利号:WO-0120995-A9
优先权日:1999-09-23
标题:Compounds directed against pilus biogenesis and activity in pathogenic bacteria; methods and compositions for synthesis thereof
发明人：KIHLBERG JAN; LARSSON ANDREAS; SVENSSON ANETTE; FEX TOMAS; HULTGREN SCOTT J; PINKNER JERRY
权利人:UNIV WASHINGTON; KIHLBERG JAN; LARSSON ANDREAS; SVENSSON ANETTE; FEX TOMAS; HULTGREN SCOTT J; PINKNER JERRY
摘要:Many Gram-negative pathogens assemble adhesive structures on their surfaces that allow them to colonize host tissues and cause disease. Novel compositions which inhibit or prevent the formation of a pilus chaperone-subunit complex are disclosed. Interfering with the function of the pili chaperone negatively affects the chaperone/usher pathway which is one molecular mechanism by which Gram-negative bacteria assemble adhesive pili structures and thus prevent or inhibit pilus assembly. Also provided are methods for the treatment or prevention of diseases caused by tissue-adhering pilus-forming bacteria by inhibiting the function of pilus chaperones. Also provided are pharmaceutical preparations capable of inhibiting or preventing the formation of a pilus chaperone-subunit complex. Also provided are methods of synthesizing the N-substituted amino acid compounds and compounds useful for the synthesis thereof. In particular, novel fluorinated linker compounds and methods of synthesis are provided. Methods for using the fluorinated linker compounds in methods of solid-phase synthesis of the N-substituted amino acid compounds are also disclosed.

专利号:US-2020354404-A1
优先权日:2019-05-09
标 题 :Peptidomimetic agents, synthesis and uses thereof
发明人：AL-ABED YOUSEF
权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH
摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.

专利号:US-5280093-A
优先权日:1989-06-29
标题 :Chiral polymers for the synthesis of pure enantiomers of amino acids
发明人：JACQUIER ROBERT; CALMES MONIQUE; DAUNIS JACQUES
权利人:RHONE POULENC CHIMIE
摘要:The present invention relates to chiral polymers and to their uses for operations of asymmetric synthesis, deracemization and optical inversion. n These polymers are characterized in that they comprise: n a chiral unit n a functionalizing unit n an optional crosslinking unit n Application to chiral organic synthesis.

专利号:US-2005214310-A1
优先权日:2004-01-23
标 题 :Melphalan prodrugs
发明人：TOKI BRIAN E; SENTER PETER D
权利人:SEATTLE GENETICS INC
摘要:Shown and described are the synthesis of more potent forms of C-Mel, a prodrug used in Antibody-Directed Enzyme Prodrug Therapy, that releases the clinically used anticancer alkylating agent melphalan extracellularly. Shown and described are the synthesis of a variety of melphalan analogues with the intention to promote facile intracellular drug access. Esters, amides, and peptides of melphalan are shown. Cephalosporin prodrugs of the most interesting melphalan derivatives were synthesized and evaluated for potency, toxicity, therapeutic window, plasma stability, and solubility.

专利号:US-2021087191-A1
优先权日:2020-12-04
标 题 :SUBSTITUTED 3-ISOBUTYL-9,10-DIMETHOXY-1,3,4,6,7,11B-HEXAHYDRO-2H-PYRIDO[2,1-a]ISOQUINOLIN-2-OL COMPOUNDS, THEIR SYNTHESIS, AND USE THEREOF
发明人：MILLER DAVE ALAN; ELLENBERGER DANIEL J; GUNIC ESMIR; GIRARDET JEAN-LUC; SPANGENBERG ANGELA
权利人:DISPERSOL TECHNOLOGIES LLC
摘要:The invention relates to substituted 3-isobutyl-9,10-dimethoxy-1,3,4,6,7,11b-hexahydro-2H-pyrido[2,1-a]isoquinolin-2-ol compounds, their synthesis, pharmaceutical compositions containing them, and methods of using them in the treatment of disorders benefiting from inhibition of vesicular monoamine transporter 2 (VMAT2).