35 results about "L-tert-leucine" patented technology

Enantiomerically pure L-tert-leucine and D-tert-leucine were prepared from (DL)-tert-leucine by diastereomeric salt formation using dibenzoyl-d-tartaric acid as the resolving agent.

The invention relates to a preparation method of MOC-L-tert-leucine, in particular to a method for preparing MOC-L-tert-leucine by resolving 2-methoxy-acylamino-3,3-dimethylbutyric acid. The method includes the steps that the 2-methoxy-acylamino-3,3-dimethylbutyric acid and a resolving agent amine compound form two kinds of diastereoisomer amine salt, then separation is performed to obtain MOC-L-tert-leucine amine salt, and then the MOC-L-tert-leucine amine salt is dissociated through acid to obtain the MOC-L-tert-leucine. The method is low in cost, simple and reasonable in technology, capable of guaranteeing high purity of the product and suitable for MOC-L-tert-leucine industrial production.

The invention relates to a new synthetic method of an HIV-1 protease inhibitor, Atazanavir, which adopts a convergent-typed synthetic strategy, introduces a construction unit, methoxycarbonyl-tert-lencyl, as an N atom protecting group in the whole early synthetic stage, and takes the diastereomeric selective reduction of aminoketone as the key and final reaction step of the new process. The method comprises the steps that: the compound of formula V, namely, N-1-[N-(methoxycarbonyl)-L-tert-leucine]-N-2-[4-(2-pyridyl)-phenmethyl]hydrazine, and the compound of formula VI, namely, (S)-1-((S)-4-chlorine-3-carbonyl-1-phenyl butane-2-yl-2-amino)-3, 3-dimethyl-1-carbonyl butane-2-yl-methyl carbamate, are treated with nucleophilic substitution reaction to generate the compound of formula VII, namely, 1-[4-(2-pyridyl)phenyl]-5(S)-2, 5-bis{[N-(methoxycarbonyl)-L-tert-leucineyl] amino}-4-carbonyl-6-phenyl-2-azahexane; and the compound of formula VII is treated with reduction reaction to generate the Atazanavir. The invention has the advantages of less process route steps, easily-controlled reaction conditions, simple and convenient operation, low-price and easily-obtained raw material, high product yield, low cost and being suitable for large-scale production.

A method for preparing atazanavir monomers applied in the field of medical technology, at an appropriate temperature, with a weak base as an acid-binding agent and a certain organic solvent, N-methoxycarbonyl-L-tert-leucine The acid first reacts with thionyl chloride to generate N-methoxycarbonyl-L-tert-leucine acid chloride, and then reacts with 1-[4-(pyridin-2-yl)-phenyl]-4(S)-hydroxy-5 (S)-2,5-diamino-6-phenyl-2-azidine was subjected to an amide reaction at room temperature to obtain atazanavir monomer. The invention has the following advantages (1) thionyl chloride is cheap, effectively reduces the cost of raw materials, and is suitable for industrialization; (2) the pollution produced is less, because it becomes soluble waste brine after post-treatment, and the environment is relatively friendly; ( 3) The operation is simple, the product yield is high, and it is easy to separate and purify, and is suitable for industrial production.

The present invention provides a L-succinylacylase consisting of: (a) a protein coded by a gene consisting of a nucleic acid sequence shown in SEQ ID No: 1; (b) a protein consisting of an amino acid sequence shown in SEQ ID No: 2; (c) a protein coded by a polynucleotide which hybridizes under a stringent condition with a nucleic acid sequence which is complementary to the nucleic acid sequence shown in SEQ ID No: 1 and having an L-succinylaminoacylase activity; or (d) a protein which consists of an amino acid sequence where one or several amino acid(s) is / are substituted, deleted, inserted and / or added in the protein consisting of the amino acid sequence shown in SEQ ID No: 2 and has an L-succinylaminoacylase activity. This enzyme is able to produce a sterically bulky unnatural amino acid such as L-tert-leucine etc. which is useful as an intermediate for pharmaceuticals.

The invention relates to a method for preparing an optical isomer by continuously resolving a nitrogenous organic compound raceme with an enzyme, and particularly relates to a method for preparing L-tert-leucine by resolution with an aminoacylase, specifically a continuous enzymatic method for producing L-tert-leucine. The method comprises the following steps: by using N-phenylacetyl-DL-tert-leucine and an inorganic alkali as raw materials and pure water as a reaction medium, preparing a substrate solution with a certain concentration; passing the substrate solution through an aminoacylase reaction column at a certain flow rate; under the enzyme catalytic actions, selectively hydrolyzing N-phenylacetyl-L-tert-leucine to generate L-tert-leucine and phenylacetic acid; and after the reaction finishes, acidifying the reaction solution, carrying out vacuum filtration to separate out unreacted N-phenylacetyl-D-tert-leucine, and separating and extracting phenylacetic acid from the filtrate with an organic solvent, wherein the L-tert-leucine is in the water phase, and the unavailable N-phenylacetyl-D-tert-leucine is racemized by high-temperature reflux and put into the resolving reaction again.

The invention relates to a preparation method of MOC-L-tertiary leucine, in particular to a method for splitting 2-methoxy group acylamino-3, 3-dimethyl butyric acid to prepare the MOC-L-tertiary leucine. Two kinds of diastereoisomer amine salt of the 2-methoxy group acylamino-3, 3-dimethyl butyric acid are formed through the 2-methoxy group acylamino-3, 3-dimethyl butyric acid and a resolving agent amine compound, MOC-L-tertiary leucine amine salt is obtained through separation, and the MOC-L-tertiary leucine is obtained by utilizing of the free acid MOC-L-tertiary leucine amine salt. The preparation method is low in cost, simple and reasonable in technique, high in product purity and suitable for industrial production of the MOC-L-tertiary leucine.

The invention discloses a method for synthesizing L-tertiary leucine through double enzymes. A coenzyme NADH is coupled and mediated by utilizing leucine dehydrogenase and isopropanol dehydrogenase, and NAD+ can be rapidly reduced into NADH through the isopropanol dehydrogenase under the action of isopropanol with the final concentration being about 10 percent in a reaction solution, so that the reaction speed is increased, the reaction time is shortened, the reaction efficiency is improved, the space time yield is increased, the amount of double enzymes is low and is not higher than 3 percent of the mass of substrates, the reaction cost is reduced, the purity of the reaction product is over 99%ee, and recrystallization and resolution are not needed.