6 results about "Annulation" patented technology

The application discloses application of a divinyl tetrazine in cyclization of a linear polypeptide, and a structure formula of the divinyl tetrazine is; the linear polypeptide has at least two free mercapto groups, and the vinyl groups of the divinyl tetrazine are subjected to Michael addition reaction with corresponding mercapto groups to form a ring. The application provides a new use of the divinyl tetrazine, the divinyl tetrazine can be subjected to high-efficiency Michael addition reaction with two natural cysteine mercapto groups on the linear polypeptide through the vinyl groups, so that double-mercapto peg cyclization of the linear polypeptide is realized, and the purpose of limiting the conformation of the linear polypeptide and improving the stability of the linear polypeptide is achieved. Moreover, the divinyl tetrazine can be subjected to a reverse electron demand Diels-Alder reaction with trans-cyclooctene (TCO) after the two vinyl groups are subjected to reaction with mercapto groups, so that functional polypeptides can be modularly constructed by coupling with functional molecules modified with TCO, and related applications are realized.

The application relates to the field of polypeptide medicine preparation, and particularly discloses a preparation method of bumenol peptide, which adopts a solid-liquid combination mode, liquid-phase synthesis of a tripeptide fragment Fmoc-Lys(Ac-Nle-Asp)-OMe, subsequent solid-phase synthesis of a cyclic heptapeptide methyl ester, cleavage, cyclization, deprotection and hydrolysis to obtain crude bumenol peptide. The cyclization site is alpha-COOH of Trp and alpha-NH2 of Lys, the reaction yield is high, and the cyclization problem between Lys and Asp in most current patents is solved. The process operation is simple, the deprotection reagent is conducive to environmental protection requirements. The crude product is easy to purify, the finished product has high yield and purity, and is suitable for industrial large-scale production.

The application provides a preparation method of an electrocatalytic SCF-substituted dihydrofuran compound, and belongs to the technical field of compound preparation. The application uses diazonium and ethylene compounds as substrates, uses an SCF source as a sulfur-containing and fluorine-containing fragment donor, realizes a one-pot cascade reaction of ring formation through electrolysis, and thus constructs the SCF-substituted dihydrofuran compound. The raw material of the application has a wide source, uses electric current as a reaction driving force, avoids or reduces the use of additional photosensitizers and chemical oxidation-reduction reagents, and has the one-pot cascade characteristics of ring C-N bond breaking, C-O bond construction, trifluoromethylation and ring formation and the like, so that the step economy can be improved.

The application discloses a preparation method of 4-[2-[(2-methoxyethoxy)methoxy]ethyl]morpholine, which comprises two steps of reactions: in the first step, triethanolamine is used as a starting material, and intramolecular dehydration and ring formation reaction occur under the action of a catalyst iron trichloride, so that an intermediate N-hydroxyethyl morpholine is obtained after rectification; in the second step, nucleophilic substitution reaction occurs between the intermediate and 2-methoxyethoxymethyl chloride in an organic solvent under the action of an acid binding agent, so that 4-[2-[(2-methoxyethoxy)methoxy]ethyl]morpholine crude product is obtained after extraction, water removal and solvent rotary evaporation, and the crude product is purified to obtain 4-[2-[(2-methoxyethoxy)methoxy]ethyl]morpholine product; the use amount of the catalyst iron trichloride in the first step is 2% to 4% of the mass of the triethanolamine; and the mass ratio of the intermediate to the 2-methoxyethoxymethyl chloride is 1:1.2 to 1.4; the product prepared by the method has a purity meeting the demand of electronic chemicals, provides a raw material basis for subsequent research in the photoresist field, and has high industrial popularization value.

The application discloses a preparation method of an intermediate of Axitinib and an intermediate of Axitinib as shown in formula VI. The application provides a preparation method of a compound as shown in formula VII, which comprises the following steps: performing ring formation reaction on a compound of formula VI in the presence of a base and a solvent to obtain the compound of formula VII. The Axitinib synthesis route provided by the application has the advantages of less steps, low cost, high purity of a synthesis product and no introduction of toxic substances.

This invention provides novel sulfate esters or salts thereof having two or more carbonyl groups, and surfactants. A compound, characterized by having the formula: R 1 -C(=O)-R 2 -C(=O)-R 3 -OSO3X represents this. (In the formula, R) 1 It is a straight-chain or branched alkyl group with 1 or more carbon atoms, or a cyclic alkyl group with 3 or more carbon atoms, wherein the hydrogen atoms bonded to the carbon atoms are not substituted or are substituted by hydroxyl groups or monovalent organic groups containing ester bonds. If it has 2 or more carbon atoms, it may contain a carbonyl group. If it has 3 or more carbon atoms, it may contain monovalent or divalent heterocycles, or it may be rolled into a ring. R 2 and R 3 Independently a single bond or a divalent linker. R 1 R 2 and R 3 The total number of carbon atoms is 6 or more. X is H, a metal atom, or NR. 4 4. Imidazolium with or without substituents, pyridinium with or without substituents, or phosphonium with or without substituents, R 4 It can be an H or an organic group, and can be the same or different. R 1 R 2 and R 3 (In this context, any two elements can bond together to form a ring.)