1420271-08-4

Usage

Uses

Used in Pharmaceutical Manufacturing:
2-Azaspiro[3.3]heptane hydrochloride is used as a pharmaceutical intermediate for the synthesis of various CNS drugs. Its unique spiro backbone and improved solubility and stability due to the hydrochloride salt form make it an essential component in the development of medications targeting neurological disorders and conditions.
Used in Medicinal Chemistry and Drug Discovery:
2-Azaspiro[3.3]heptane hydrochloride is utilized as a key building block in medicinal chemistry for the design and synthesis of novel compounds with potential therapeutic applications. Its versatile chemical structure allows for the exploration of new drug candidates, contributing to the advancement of drug discovery efforts in various therapeutic areas.

Upstream product

• 5445-51-2 cyclobutane-1,1'-dicarboxylic acid 
• 4415-73-0 [1-(hydroxymethyl)cyclobutyl]methanol 
• 64936-58-9 cyclobutane-1,1-diylbis(methylene)dimethanesulfonate 
• 1259489-92-3 N-Boc-2-azaspiro[3,3]heptane 

Relevant academic research and scientific papers

Method for mildly preparing 2-azaspiro [3.3] heptane hydrochloride

The invention relates to a method for mildly preparing 2-azaspiro [3.3] heptane hydrochloride, and solves the technical problem that in historical literatures, harsh conditions of strong base sodium are needed. The synthesis method comprises the following steps: (1) reducing cyclobutane-1,1-dicarboxylic acid into dimethyl alcohol; (2) reacting the 1, 1-cyclobutane dimethyl carbinol with methanesulfonyl chloride to generate 1,1-cyclobutane dimethyl carbinol dimethyl sulfonate; (3) carrying out ring closing on the 1,1-cyclobutane dimethyl carbinol dimethyl sulfonate and the 2-nitrobenzene sulfonamide to generate 2-(2-nitrobenzenesulfonyl)-2-azaspiro [3.3] heptane; (4) enabling the 2-(2-nitrobenzenesulfonyl)-2-azaspiro [3.3] heptane to react with dodecanethiol under the action of DBU to remove the 2-nitrobenzenesulfonyl so as to generate 2-azaspiro [3.3] heptane; and (5) reacting the 2-azaspiro [3.3] heptane with BOC anhydride to generate Boc-2-azaspiro [3.3] heptane, and then performing treatment with hydrochloric acid to obtain the 2-azaspiro [3.3] heptane hydrochloride. The method is mild and easy to operate, and avoids violent conditions of removing amino protecting groups by strong base at high temperature.

Tigecycline derivatives (by machine translation)

The invention belongs to the medicinal technical field, and in particular relates to a tigecycline derivative of general formula (I), a pharmaceutically acceptable salt, precursor drug, solvate or isomer thereof, wherein R2a, R2b, R3, R4a, R4b, R5, R6a, R