40 results about "Dieckmann condensation" patented technology

The invention discloses a preparation method of 3-quinuclidinone hydrochloride, which comprises the following steps: carrying out temperature control reaction on 4-picolinic acid and chloroacetic acid under alkaline water conditions to obtain an aqueous solution of a compound a, and directly entering the next reaction without post-treatment after the reaction is finished; adding a reducing agent alkaline water system into the aqueous solution of the compound a, controlling the temperature to react, controlling the temperature to adjust the pH value to 5-5.5 after the reaction is finished, extracting with n-butyl alcohol, and drying to obtain an n-butyl alcohol solution of a compound b, and directly entering the next reaction step; wherein the reducing agent is one of sodium borohydride and potassium borohydride; dropwise adding thionyl chloride into an n-butyl alcohol solution of the compound b, controlling the temperature to react after dropwise adding is ended, and concentrating to remove the solvent and unreacted thionyl chloride after the reaction is ended, so as to obtain a compound c; carrying out Dieckmann condensation reaction on the compound c at controlled temperature under the condition of organic alkali by using toluene as a solvent, carrying out hydrochloric acid quenching reaction after the reaction is finished, and directly carrying out next-step reaction after extracting and removing impurities from a water phase containing a hydrochloride solution of a compound d by using toluene; and carrying out a decarboxylation reaction on the compound d in a hydrochloric acid aqueous solution at controlled temperature, after the reaction is finished, adjusting the pH value to 10-13, extracting, and salifying to obtain a target compound TM, namely 3-quinuclidinone hydrochloride. The preparation method of 3-quinuclidinone hydrochloride provided by the invention has the advantages of economical and easily available raw materials, mild reaction conditions, efficient reaction, simple operation and low cost, and is suitable for industrial application.

The invention belongs to the technical field of medicine preparation, and particularly relates to 6-phenyl-purine derivatives as well as a preparation method and medical application thereof. The structural formula of the 6-phenyl-purine derivative is shown in the specification. The preparation method of the 6-phenyl-purine derivative comprises the following steps: S1, carrying out substitution reaction on R1-CH2NH2 and a compound 1 under the catalysis of organic base to obtain a compound 2; s2, carrying out Dieckmann condensation reaction on the compound 2 and excessive CDI to obtain a compound 3; s3, the compound 3 and phenylboronic acid are subjected to a Suzuki coupling reaction under catalysis of sodium carbonate, Pd (OAc) 2 and TPPTS, and the 6-phenyl-purine derivative with the structure shown in the general formula I is obtained. The 6-phenyl-purine derivative has antineoplastic activity and can be applied to preparation of antineoplastic drugs.

The invention belongs to the field of medicines, and discloses pyrimido imidazolone derivatives as well as a preparation method and medical application thereof. The pyrimidino imidazolone derivative has a structure as shown in a general formula I. The preparation method comprises the following steps: carrying out substitution reaction on 1-(4-methoxyphenyl)-1-R2-methylamine and a compound 1 under the catalysis of an organic base to obtain a compound 2; carrying out Dieckmann condensation reaction on the compound 2 and excessive CDI to obtain a compound 3; and carrying out Suzuki coupling reaction on the compound 3 and different substituted arylboronic acid or morpholine under the catalysis of sodium carbonate, Pd (OAc) 2 and TPPTS to obtain the pyrimido imidazolone derivative. The pyrimido imidazolone derivative selectively has a strong inhibition effect on proliferation of tumor cells of lung cancer, prostatic cancer, colon cancer, breast cancer, liver cancer and the like, and can be applied to preparation of medicines for treating and / or preventing malignant tumors.