The invention relates to a preparing method of N-t-butyloxycarboryl-4-nitro piperidine. The method mainly solves the technical problems that in an existing synthetic process, the route is long, yield is low, reaction is not easy to control, experimental operation is inconvenient, and the like. According to the method, N-t-butyloxycarboryl-4-hydroxy piperidine is used as raw material to prepare N-t-butyloxycarboryl-4-iodine piperidine, and further the target product is obtained through the substitution reaction. The N-t-butyloxycarboryl-4-nitro piperidine obtained with the method is a useful intermediate or product used for synthesis of various kinds of drugs.

Preparing method of N-t-butyloxycarboryl-4-nitro piperidine

The invention relates to a synthesis method of a compound of 7-hydroxymethyl-2,5-diazaspiro [3,4] octane-2-dimethylethylester, and mainly solves the technical problem that no industrial method suitable for industrial synthesis exists in the prior art. A compound 1 and triethyl-phosphite are used as raw materials for synthesizing and obtaining the final compound through eight steps. A reaction formula is shown in the specification.

Synthesis method of 7-hydroxymethyl-2,5-diazaspiro [3,4] octane-2-dimethylethylester

The invention discloses a method for synthesis of the bicyclic compound 1,8-diazaspiro [4,5] decane-3-hydroxy-1-benzyl-8-carboxylic acid tert-butyl ester. The raw material N-Boc-4-piperidone easy to obtain is adopted, and the 1,8-diazaspiro [4,5] decane-3-hydroxy-1-benzyl-8-carboxylic acid tert-butyl ester is obtained through dehydration condensation reaction, allyl Grignard addition reaction, epoxidation reaction and proton abstraction ring-closing reaction which are conducted continuously.

Method for synthesis of 1,8-diazaspiro [4,5] decane-3-hydroxy-1-benzyl-8-carboxylic acid tert-butyl ester

The invention relates to a preparation method of 1-benzyl-8-tert-butyl-2-hydroxymethyl-1,8-diazaspirane[45]decane-1,8-dicarboxylate, mainly aiming at solving the technical problem that a suitable industrial synthesis method does not exist at present The preparation method comprises six steps: firstly, taking a compound 1 and oxalyl chloride to react in dichloromethane, so as to generate a compound 2; then obtaining a compound 3 under the action of triethylamine; then taking the compound 3 to react with a vinyl Grignard reagent, so as to obtain a compound 4; then taking the compound 4 and a compound 5 to react under the condition that DBU is used as alkali, so as to obtain a compound 6; carrying out hydrogenation ring closure to obtain a compound 7; finally, taking the compound 7 to react with benzyl chloroformate under an alkaline condition, so as to obtain a final product 8 The compound prepared by the preparation method is used as a useful intermediate or product for synthesizing various medicines

Preparation method of 1-benzyl-8-tert-butyl-2-(hydroxymethyl)-diazaspirane decane dicarboxylate

The invention relates to a method for preparing 1,8-diazaspiro[4.5]decane with a protective group, and mainly solves the technical problems that the conventional synthetic route for the 1,8-diazaspiro[4.5]decane is long, the yield is low, an intermediate is difficult to purify, reaction conditions are rigorous, and mass production cannot be performed. The method comprises the following steps of: performing Michael addition reaction on N-PG-4-nitropyridine serving as a raw material and acrylic ester in alcoholic solution or acetonitrile to obtain N-PG-4-propanal-4-nitropyridine; and adding a catalyst into the product in an organic solvent, and performing hydrogenation reduction ring-closing reaction to obtain the 1,8-diazaspiro[4.5]decane with the protective group. The method has the advantages of a few reaction steps, high yield and mild conditions, and is a synthetic method with large-scale preparation value.

Method for synthesizing 1,8-diazaspiro[4.5]decane with protective group

Method for synthesizing 1,7-diazaspiro[4.5]decane with protective group

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Method for synthesizing 1,8-diazaspiro[4.5]decane with protective group

Method for synthesizing 1,7-diazaspiro[4.5]decane with protective group