CAS: 26782-71-8; H-D-Tle-Oh

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33105-81-6 132684-60-7 20859-02-3

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3,3-二甲基-1-丁酸置于磷化氢,氨,氯,Sodium Hydroxide体系中,用 Aq. Phosphate Buffer,水 用作溶剂,130.0 °C,14.53 Kpa 条件下,反应 16.0H,反应生成D-叔亮氨酸
参考文献:一种同时制备d-和l-型叔亮氨酸的方法
标题:一种同时制备d-和l-型叔亮氨酸的方法
摘要:本发明公开了一种同时制备d-和l-型叔亮氨酸的方法,包括以下步骤:步骤(1):将正丁醇与1,1-二氯乙烯反应,得到3,3-二甲基丁酸产物;步骤(2):在3,3-二甲基丁酸产物中加入催化剂,同时通入空气和氯气,进行氯代,得到2-氯-3,3-二甲基丁酸;步骤(3):将得到的2-氯-3,3-二甲基丁酸进行氨解反应,得到d-,L-叔亮氨酸;步骤(4):对得到的d-,L-叔亮氨酸进行乙酰化和氯乙酰化,让后用l-热稳定氨基酸酰化酶拆分和其它处理,分别得到l-叔亮氨酸和d-叔亮氨酸;步骤(5):将拆分回收的乙酰化或氯乙酰化回收d-叔亮氨酸进行消旋,再进行循环拆分.本发明使用了成本低廉的正丁醇和1,1-二氯乙烯为起始原料.从经济效益上讲,本发明成本显著低于生物还原法.

专利信息

专利号:WO-8800592-A1
优先权日:1986-07-18
标题:DIASTEROSELECTIVE STRECKER SYNTHESIS OF alpha-AMINOACIDS FROM GLYCOSYLAMINE DERIVATES
发明人：KUNZ HORST; SAGER WILFRIED; PFRENGE WALDEMAR; DECKER MATHIAS
权利人:CELAMERCK GMBH & CO KG
摘要:O-acyl-protected glycosylamines, in particular 2,3,4,6-tetra-O-pivaloyl-beta-D-galactopyranosylamine (1), their preparation and their use for the diastereoselective synthesis of alpha-aminoacids. With compounds such as (1), one can obtain by Strecker synthesis high yields and high diastereomer surplus. The direction of the asymmetric induction can be determined by the selection of the solvent. This type of synthesis is particularly effective when carried with Lewis acid catalysts. One obtains also high yields and high diastereoselectivity during Ugi four component synthesis facilitated by Lewis acids by using amines such as (1).

专利号:US-8680294-B2
优先权日:2009-07-29
标题 :Enantio- and stereo specific synthesis of β-amino-α-hydroxy amides
发明人：TRAVERSE JOHN; LEONG WILLIAM M; MILLER STEVEN P; ALBANEZE-WALKER JENNIFER; HUNTER THOMAS J; WANG LIJUN; LIAO HONGBIAO; ARASAPPAN ASHOK; TRZASKA SCOTT T; SMITH RANDI M; LEKHAL AZZEDDINE; BOGEN STEPHANE L; KONG JIANSHE; BENNETT FRANK; NJOROGE F GEORGE; POIRIER MARC; KUO SHEN-CHUN; CHEN YONGGANG; MATTHEWS KENNETH S; DEMONCHAUX PATRICE; FERREIRA AMADEO
权利人:TRAVERSE JOHN; LEONG WILLIAM M; MILLER STEVEN P; ALBANEZE-WALKER JENNIFER; HUNTER THOMAS J; WANG LIJUN; LIAO HONGBIAO; ARASAPPAN ASHOK; TRZASKA SCOTT T; SMITH RANDI M; LEKHAL AZZEDDINE; BOGEN STEPHANE L; KONG JIANSHE; BENNETT FRANK; NJOROGE F GEORGE; POIRIER MARC; KUO SHEN-CHUN; CHEN YONGGANG; MATTHEWS KENNETH S; DEMONCHAUX PATRICE; FERREIRA AMADEO; MERCK SHARP & DOHME
摘要:Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.

专利号:US-2023037284-A9
优先权日:2018-11-30
标题:Combination therapy of peptidomimetic macrocycles
发明人：GUERLAVAIS VINCENT; ANNIS DAVID ALLEN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.

专利号:US-9574189-B2
优先权日:2005-12-01
标题:Enzymatic encoding methods for efficient synthesis of large libraries
发明人：FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK
权利人:FRANCH THOMAS; LUNDORF MIKKEL DYBRO; JACOBSEN SØREN NYBOE; OLSEN EVA KAMPMANN; ANDERSEN ANNE LEE; HOLTMANN ANETTE; HANSEN ANDERS HOLM; SØRENSEN ANDERS MALLING; GOLDBECH ANNE; DE LEON DAEN; KALDOR DITTE KIEVSMOSE; SLØK FRANK ABILDGAARD; HUSEMOEN GITTE NYSTRUP; DOLBERG JOHANNES; Jensen Kim Birkebæ; PEDERSEN LENE; NØRREGAARD-MADSEN MADS; GODSKESEN MICHAEL ANDERS; GLAD SANNE SCHRØDER; NEVE SØREN; THISTED THOMAS; KRONBORG TINE TITILOLA AKINLEMINU; SAMS CHRISTIAN KLARNER; FELDING JAKOB; FRESKGÃ…RD PER-OLA; GOULIAEV ALEX HAAHR; PEDERSEN HENRIK; NUEVOLUTION AS
摘要:Disclosed is a method for obtaining a bifunctional complex comprising a molecule linked to a single stranded identifier oligonucleotide, wherein a nascent bifunctional complex comprising a chemical reaction site and a priming site for enzymatic addition of a tag is a) reacted at the chemical reaction site with one or more reactants, and b) reacted enzymatically at the priming site with one or more tag(s) identifying the reactant(s).

专利号:US-2025084410-A1
优先权日:2015-01-12
标 题:Incorporation of unnatural nucleotides and methods thereof
发明人：PTACIN JEROD; MALYSHEV DENIS A; CAFFARO CAROLINA E
权利人:SYNTHORX INC
摘要:Disclosed herein are methods, compositions and kits for the synthesis of proteins which comprises unnatural amino acids that utilize a mutant tRNA.

专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.