Abstract:
Disclosed is a method for the production of an optically active amine compound. The method is characterized by converting a ketone compound to a corresponding optically active amine compound by using an amino transferase (A), an a-keto acid reductase (B) and an enzyme (C) each having a specific property in a single of reaction system, wherein a carbon atom to which an amino group is attached in the optically active amine compound is an asymmetric point. Also disclosed is a recombinant vector for use in the method. It becomes possible to produce an optically active amine compound with high efficiency.
Abstract:
A process for the production of an optically enriched tertiary alcohol of the formula (2a) or (2b), by reacting an epoxide of the formula (1) with a nucleophilic agent Nu in the presence of halohydrin dehalogenase.
Abstract:
A method for enzymatically synthesizing a polymer by combining a preselected quantity of an enzyme, a first reactant selected from polymers with at least one carboxylic acid pendant group, a second reactant selected from alcohols, i.e., polyols, in a reaction vessel; heating the reaction vessel to a preselected temperature; and maintaining the reaction vessel at the preselected temperature for a preselected time with mixing, wherein an esterification reaction results at at least one carboxylic acid pendant group of the polymer with one hydroxyl group from the polyol and results in a modified polymer.
Abstract:
Treatment of a racemic lactate derivative with an enzyme having an ability to hydrolyze an ester asymmetrically causes specific hydrolysis of the ester moiety of one of the optical isomers constituting the racemic lactate derivative, and use of the resulting hydrolyzate as an intermediate enables the preparation of an optically active propoxyaniline derivative in a decreased number of steps as compared with the prior art. (A)
Abstract:
Process for the preparation of an enantiomerically enriched acylated amine, wherein an enantiomerically enriched, substituted or unsubstituted phenylglycine amide is contacted with a mixture of enantiomers of the corresponding amine H2NCR1R2R3 where R1, R2 and R3 are not the same and each independently stands for H, CN, a substituted (cyclo)alkyl group, aryl group, alkylaryl group or arylalkyl group, a cyclic or non-cyclic heteroaryl group or heteroaryl group with one or more N, O of S atoms or (CH2)n-COR4, where n=0, 1 ...6 and R4 is OH or a substituted or unsubstituted alkyl group, aryl group, alkoxy group or amino group or where R1 and R2 (and R3) together with the C atom to which they are bound form a (bi)cyclic group which may or may not contain one or more N, O of S atoms, in the presence of a Pen-G acylase. A process for the preparation of enantiomerically enriched amine with formula H2NCR1R2R3 where R1, R2 and R3 are as defined above, wherein an acylated amine is contacted with a Pen-G acylase. Preferably a Pen-G acylase derived from Alcaligenes faecalis is applied.
Abstract translation:制备对映异构体富集的酰化胺的方法,其中将对映异构体富集的取代或未取代的苯基甘氨酸酰胺与相应的胺H 2 NCR 1 R 2 R 3的对映异构体的混合物接触,其中R1,R2和R3不相同,并且各自独立地代表H, CN,取代的(环)烷基,芳基,烷基芳基或芳烷基,具有一个或多个S原子或(CH 2)n-COR 4的N,O的环状或非环状杂芳基或杂芳基,其中n = 0,1 ... 6,R4是OH或取代或未取代的烷基,芳基,烷氧基或氨基,或者其中R1和R2(和R3)与它们所结合的C原子一起形成( bi)环基团,其可以含有或不含有一个或多个S原子的N,O,在Pen-G酰基转移酶存在下。 制备具有式H2NCR1R2R3的对映异构体富集的胺的方法,其中R1,R2和R3如上定义,其中酰化的胺与Pen-G酰基转移酶接触。 优选地,应用来自产碱杆菌的Pen-G酰基转移酶。
Abstract:
The present invention relates to isolated polypeptides with lipase activity, selected from the group consisting of:(a)a polypeptide having at least 75%, at least 80%, at least 85%, at least 90%, at least 91%, at least 92%, at least 93%, at least 94%, at least 95%, at least 96%, at least 97%, at least 98%, at least 99%, or 100% sequence identity to SEQ ID NO: 4;(b)a polypeptide encoded by a polynucleotide that hybridizes under low stringency conditions, medium stringency conditions, medium-high stringency conditions, high stringency conditions, or very high stringency conditions with (i) SEQ ID NO: 3or the full-length complement of (i);(c)a polypeptide encoded by a polynucleotide having at least 75%, at least 80%, at least 85%, at least 90%, at least 91%, at least 92%, at least 93%, at least 94%, at least 95%, at least 96%, at least 97%, at least 98%, at least 99%, or 100% sequence identity to SEQ ID NO: 3;(d)a polypeptide which is a variant of SEQ ID NO: 4 comprising a substitution, deletion, and/or insertion at one or more (e.g. several) positions; and(e)a polypeptide which is a fragment of any of the polypeptides of (a), (b), (c) or (d).The invention also relates to polynucleotides encoding the polypeptides; nucleic acid constructs, vectors, and host cells comprising the polynucleotides; and methods of using the polypeptides.
Abstract translation:本发明涉及具有脂肪酶活性的分离的多肽,其选自:(a)多肽,其具有至少75%,至少80%,至少85%,至少90%,至少91%,在 与SEQ ID NO:4的至少92%,至少93%,至少94%,至少95%,至少96%,至少97%,至少98%,至少99%或100%的序列同一性 ;(b)由多核苷酸编码的多肽,其在低严格条件,中等严格条件,中等严格条件,高严格条件或非常高严格条件下与(i)SEQ ID NO:3或全长补体 (c)由多核苷酸编码的多肽,所述多核苷酸具有至少75%,至少80%,至少85%,至少90%,至少91%,至少92%,至少93% 与SEQ ID NO:3的至少94%,至少95%,至少96%,至少97%,至少98%,至少99%或100%的序列同一性;(d) SEQ ID NO:4的变体包含取代, 和/或插入在一个或多个(例如, 几个)职位; (e)多肽,其是(a),(b),(c)或(d)的多肽的片段。本发明还涉及编码多肽的多核苷酸; 核酸构建体,载体和包含多核苷酸的宿主细胞; 和使用多肽的方法。
Abstract:
The present invention relates to processes for the preparation of 5-methyl-3-nitromethyl-hexanoic acid ester and its salts. Also disclosed are processes for the preparation of 5-methyl-3-nitromethyl-hexanoic acid salt and a process for the preparation of 3-(aminomethyl)-5- methylhexanoic acid. (S)-5-Methyl-3-nitromethyl-hexanoic acid or (R)-5-methyl-3-nitromethyl-hexanoic acid in enantioenriched form or enantiopure form as well as salts thereof, (S)-5-methyl-3-nitromethyl-hexanoic acid ester or (R)-5-methyl-3-nitromethyl-hexanoic acid ester in enantioenriched form or enantiopure form and a compound, namely Formula (XIII), in racemic form, enantioenriched form or enantiopure form are also disclosed.
Abstract:
A novel process of preparation of racemic pregabalin from comprising an intermediate of structure 111 comprising reductive ring opening to form a structure IV followed few alternative routes that yield racemic pregabalin that is resolved to yield (S) + pregabalin by using chemical or enzymatic methods. A new chemical entity of structure IHc li|c is also disclosed as a novel intermediate. A part of the novel process also comprises a new process of producing a compound of structure VII comprising acylation of compound of structure V followed by elimination and improving a process of producing a compound of structure VII comprising reacting isovaleraldehyde with nitromethane through the compounds 4-methyl-1-nitropentan- 2-ol, 3-methyl-1-(nitromethyl)butylacetate, and 3-methyl-1-(nitromethyl)butyl acetate under suitable conditions to 4-methyl-1-nitropet-1-ene. Enzymatic processes of resolution of racemic pregabalin esters into (S) pregabalin and (R) pregabalin are also disclosed.
Abstract translation:一种制备外消旋普瑞巴林的新方法,包括结构111的中间体,其包含还原性环开口以形成结构IV,其次是产生外消旋普瑞巴林的替代路线,其通过使用化学或酶学方法被分离产生(S)+普瑞巴林。 结构IHc li | c的新化学实体也被公开为新型中间体。 新方法的一部分还包括生产结构VII化合物的新方法,包括结构化V化合物的酰化,随后消除并改进制备结构VII化合物的方法,包括使异戊醛与硝基甲烷反应,通过化合物4-甲基 -1-硝基丙-2-醇,3-甲基-1-(硝基甲基)丁酸乙酯和3-甲基-1-(硝基甲基)乙酸丁酯在适当条件下反应,得到4-甲基-1-硝基-1-烯。 还公开了将外消旋普瑞巴林酯分解成(S)普瑞巴林和(R)普瑞巴林的酶学方法。
Abstract:
A process for easily producing optically active alcohols which are (R)-3-hydroxypentanenitrile, an optically active 3-hydroxybutanoic ester, and an optically active 1-phenylethanol derivative; and a novel enzyme useful for the production of the optically active alcohols, in particular, (R)-3-hydroxypentanenitrile. The enzyme is a novel acetoacetyl-CoA reductase which is capable of asymmetrically reducing 3-ketopentanenitrile to produce (R)-3-hydroxypentanenitrile having an optical purity of 99% e.e. or higher. The process comprises causing the novel enzyme or a known acetoacetyl-CoA reductase to act on each of 3-ketopentanenitrile, an acetoacetic ester, and a 1-phenylethanone derivative to produce the corresponding optically active alcohols.
Abstract:
Die vorliegende Erfindung betrifft Proteine, die eine enzymatische Aktivität zur Reduktion von substituierten Alkanonen, wie 3-Methylamino-1-(2-thienyl)-propan-1-on, aufweisen. Die Erfindung betrifft weiterhin Nukleinsäuren, die für diese Proteine kodieren, Nucleinsäurekonstrukte, Vektoren, genetisch veränderte Mikroorganismen sowie Verfahren zur Herstellung von substituierten (S)-Alkanolen, wie z.B. (S)-3-Methylamino-1-(2-thienyl)-(S)-propanol.