Compounds for regulating nmda receptor activity, pharmaceutical compositions and uses thereof
A compound and composition technology, applied in the field of compounds that regulate NMDA receptor activity, can solve the problems of addiction-induced dissociation, Rapastinel cannot be taken orally, and limited clinical application
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preparation example 1
[0104] Preparation Example 1: Synthesis of L-thiazolidinic acid
[0105]
[0106] Dissolve 12.1g (0.1mol) of L-cysteine in 60ml of hot water, slowly pour into 10mL of 36% formaldehyde aqueous solution, shake well and let it stand overnight, filter the precipitated crystals the next day, and then wash with ethanol and water Recrystallization gave 12.8 g of needle-like white crystals, with a yield of 96.2%.
preparation example 2
[0107] Preparation Example 2: Synthesis of L-thiazolidinic acid methyl ester hydrochloride
[0108]
[0109] Dissolve 13.3 g (0.1 mol) of L-thiazolidinic acid in 100 ml of anhydrous methanol, pass hydrogen chloride gas until the raw materials are completely dissolved, continue to ventilate for more than 2 hours, and stir overnight after ventilating. The next day, the solvent was evaporated to dryness under reduced pressure, and the residue was dissolved in methanol and evaporated to dryness again. This was repeated twice to take away hydrogen chloride gas. The solvent was evaporated to dryness to obtain the crude product, which was recrystallized from methanol-ether with a yield of 91%.
preparation example 3
[0110] Preparation Example 3: Synthesis of N-tert-butoxycarbonyl-L-thiazolidinic acid
[0111]
[0112] Under ice bath, dissolve 0.10mol of L-thiazolidinic acid in 50mL of 2N aqueous sodium hydroxide solution (0.10mol), and mix 24.4g (0.11mol) of tert-butoxycarbonyl anhydride and 50mL of acetone with stirring Slowly added dropwise, and continued to stir for 2h. Add 200 mL of water to dilute the reaction solution, and extract 3 times with ethyl acetate, each time with 80 mL of ethyl acetate; discard the organic phase. The aqueous phase was adjusted to pH 2 with 1 mol / L hydrochloric acid in an ice bath, and extracted three times with ethyl acetate, each time using 80 mL of ethyl acetate; the organic phases were combined, dried over anhydrous sodium sulfate, and the solvent was removed under reduced pressure, and White crystals were obtained by recrystallization from petroleum ether and ethyl acetate with a yield of 88%.
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