专利号:US-6350595-B1 优先权日:1997-10-28 标题:Synthesis of polynucleotides having random sequences 发明人:NEUNER PHILIPPE 权利人:ISTITUTO DI RICERCHE DI MOLECO 摘要:Subject of this invention is a process for the chemical synthesis of polynucleotides having totally or partially random sequences, based on the utilization, as synthesis monomer units for the random sequence part, or presynthesized mononucleotides and dinucleotides. Said synthesis is carried out on separate supports, so that on each of those supports is alternated at least one reaction cycle wherein a mixture of said dinucleotides is bound, with at least one reaction cycle wherein a mononucleotide is bound, and that in a preferred embodiment at the end of the n cycles required for a codon synthesis, the supports are mixed and then redivided into one or more reaction containers. The resulting polynucleotides are such that, for the random sequence part, each trinucleotide unit is fit to match only a limited number of codons, predefined for each unity in number and sequence, and the genetic code degeneracy effects can thus be eliminated. FIG. 1 shows the chemical structure of the dinucleotides utilized as monomer units for the synthesis of codons forming the final sequence.
专利号:WO-9312076-A1 优先权日:1991-12-13 标题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS ROY 权利人:CORVAS INT INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-2024035023-A1 优先权日:2022-06-24 标题 :Computer implemented method for engineering fluorinase enzymes for synthesis of fluorophenyl compounds 发明人:R PRAVIN KUMAR; G GLADSTONE SIGAMANI; L ROOPA; B K NAVEEN; SHETTY ANUJ J; M LIKITH 权利人:KCAT ENZYMATIC PRIVATE LTD 摘要:The present invention discloses a computer-implemented method for engineering fluorinase enzymes towards the synthesis of fluorophenyl compounds. Limited or no mechanistic details of fluorinase enzymes have hindered progress in understanding their catalytic mechanisms for synthesizing synthetic organofluorine compounds. Through a comprehensive computational screening process, specific methionine-sulfonium phenyl substrates, including [(3S)-3-amino-3-carboxypropyl][2,5-difluoro-4-(4-methoxy-2,4-dioxobutyl)phenyl]methylsulfonium, were designed and optimized using quantum chemical optimization techniques. This methodology uncovers crucial information on F— ion attack conformation and the catalytic mechanism of the substrate, leading to the formation of Methyl 3-oxo-4-(2,4,5-trifluorophenyl)butanoate. Furthermore, a protein sequence and 3D modeling-based enzyme screening process was employed to identify the most suitable enzyme for this substrate. The identified enzyme was then engineered using the mechanistic insights gained from the studies, resulting in improved substrate scope, stability and catalytic efficiency. This computer-based approach offers an efficient and precise alternative to traditional trial-and-error methods, advancing the field towards the successful synthesis fluorophenyl compounds.
专利号:US-2025019732-A1 优先权日:2023-07-07 标 题:Method for chemical-biological cascade synthesis of l-phosphinothricin and mutants therefor 发明人:XUE YAPING; CHENG FENG; ZOU SHUPING; XU JIANMIAO; ZHENG YUGUO 权利人:UNIV ZHEJIANG TECHNOLOGY 摘要:A method for chemical-biological cascade synthesis of L-phosphinothricin is carried out as follows: 3-(methylethoxyphosphinyl) ethyl propionate is synthesized by addition reaction from diethoxymethylphosphine and acrylic acid, then a condensation reaction is carried out with 3-(methylethoxyphosphinyl) ethyl propionate and sodium ethoxide as reactants, then the product is subjected to a hydrolysis reaction with diethyl oxalate to synthesize 4-(hydroxymethylphosphinyl)-2-oxobutyric acid, and finally, L-phosphinothricin is catalytically synthesized by taking 4-(hydroxymethylphosphinyl)-2-oxobutyric acid as a raw material, and using highly active and stable wet cells co-expressing phsophinothricin dehydrogenase and alcohol dehydrogenase or co-expressing a phsophinothricin dehydrogenase mutant and alcohol dehydrogenase as a biocatalyst, thereby solving the problems of existing L-phosphinothricin synthesis being tedious, low asymmetric amination reduction activity and poor stability.
专利号:US-5283293-A 优先权日:1990-12-14 标 题:Reagents for automated synthesis of peptide analogs 发明人:WEBB THOMAS R 权利人:CORVAS INC 摘要:Reagents suitable for synthesis of peptide analogs using automated peptide synthesis and procedures for synthesis of peptide analogs are provided.
专利号:US-7294486-B2 优先权日:2001-09-05 标 题:Enzymatic process for the synthesis of organo-fluorine compounds 发明人:O'HAGAN DAVID; SCHAFFRATH CHRISTOPH 权利人:UNIV ST ANDREWS 摘要:There is described a process for the synthesis of a fluoronucleoside compound, said process comprising mixing a substrate and an enzyme from Streptomyces cattelya as catalyst. The process may be used to produce an 18 F labelled fluoronucleoside compound. There is also described an enzyme derived from Streptomyces cattelya which has the capacity to catalyse the synthesis of a fluoronucleoside compound.
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