35results about How to "Short route steps" patented technology

The invention provides an elagolix synthesis method. The elagolix synthesis method comprises enabling a compound 5 and a compound 10 to participate in a condensation reaction to finish N-alkylation reaction to obtain a compound 11, and then implementing alkaline hydrolysis to obtain elagolix 12. The invention further discloses two synthesis methods of the compound 5: the method I comprises enabling a 5-bromine-6-methylpyrimidine-2,4(1H,3H)-diketone compound 1 and a 2-(brooethyl)-1-fluorin-3-(trifluoromethyl) benzene compound 2 to have a condensation reaction to obtain an intermediate 3, and then having a coupling reaction; the method II comprises enabling 1-halide-3-fluorin-2-anisole and acetoacetate 7 to have a coupling reaction to obtain a compound 8, and then having a condensation cyclization reaction with a compound 9; the improvements greatly shorten the route steps, the route efficiency is improved, the use of a noble metal catalyst is avoided, and the process cost is greatly lowered. The operation of the route is simple, the total yield is high, the purity of an obtained product is also relatively high, and the method is suitable for the enlarged production.

The invention discloses new intermediate compounds 6 and 7 of bempedoic acid, and also discloses a synthetic method of bempedoic acid. The method shortens the route steps, improves the yield, lowers the process cost, improves the structure of the bempedoic acid intermediate, enhances the crystallinity of the intermediate compounds, and is beneficial to enhancing the purity of the final product, and suitable for enlarged production. The structural formulas of the compound 6 and the compound 7 are shown in the specification, wherein -N(R2)2 represents N,N-dimethylamino, cyclohexylamino, morpholinyl or amino; and M is an inorganic base or organic alkali, and comprises sodium, potassium, calcium, cyclohexanediamine or morpholine.

The invention discloses a preparation method of pramipexole dihydrochloride and an intermediate thereof. The invention provides a preparation of pramipexole II. The preparation method of the pramipexole II comprises the following steps: performing condensation reaction and reduction reaction on a pramipexole intermediate III, propylamine and hydrogen in an organic solvent and under the existence of a chiral catalyst, and performing one-pot method to obtain the pramipexole II. According to the preparation method provided by the invention, the route step is short, chiral resolution is not neededand the total molar yield is high; furthermore, the prepared product has high purity, can reach to the standard of raw material medicines and is suitable for industrialized production. (The formula is shown in the description).

The invention discloses a preparation method of tebipenem ester. The method comprises the following steps of: 1), carrying out reaction on the compound of the formula (IV) under acidic or alkaline condition, removing protective groups, so as to obtain tebipenem acid, wherein the pH (potential of hydrogen) value of the acidic condition is 2-6 and the pH value of the alkaline condition is 9-13; and 2), reacting the tebipenem acid with iodomethyl pivalate, so as to obtain the tebipenem ester. The method disclosed by the invention is easy to operate and mild in reaction condition, the noble metal palladium catalyst is not required, and thus the method is more beneficial for industrial production and the cost is greatly reduced. Formula (IV) is shown in the specification.

The invention discloses a preparation method of odanacatib, and a preparation method of an odanacatib intermediate. The preparation method of the trifluoroethylketone biphenyl methylsulfone intermediate I comprises the following step: 2,2,2-trifluoro-1-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl]ethanone and 4-bromophenyl methyl sulfone undergo a coupling reaction in a solvent in the presence of a metal catalyst and an inorganic alkali to obtain the trifluoroethylketone biphenyl methylsulfone intermediate I. The preparation methods have the advantages of simplicity and safety in operation, short route steps, environmental friendliness, high reaction yield, and high purity of the obtained products, and the odanacatib II obtained by using the trifluoroethylketone biphenyl methylsulfone intermediate I as the intermediate has the advantages of high purity, meeting of bulk drug standards, and suitableness for industrial production.

The invention belongs to the field of medical chemistry, and relates to a preparation method of a quinoline TGF-beta1 inhibitor, in particular to a preparation method of 4-((1-cyclopropyl-3-(tetrahydro-2H-pyran-4-yl)-1H-pyrazole-4-yl) oxy)-7-(3-(trifluoromethyl)-5, 6-dihydro-[1, 2, 4] triazolo [4, 3-a] pyrazine-7 (8H)-yl) quinoline as shown in a formula (I) or a salt, a hydrate, a solvate or a crystal thereof.

The invention discloses a method for synthesizing aromatic primary amine through OTF amination. Amination reaction is carried out on OTF of an aromatic group and benzophenone imine, and then benzhydryl is removed to obtain an aromatic primary amine compound. According to the method for synthesizing the primary aromatic amine through OTF amination, the raw materials are cheap and easy to obtain, the preparation cost is greatly reduced, meanwhile, the operation condition is mild, the operation difficulty is reduced, the energy consumption is low, no pollution is caused to the environment, and the method is suitable for green and environment-friendly industrial production and beneficial to enlarged production and industrial popularization.