PREPARATION METHOD OF PILOCARPINE AND ITS INTERMEDIATE COMPOUNDS

    公开(公告)号:US20240228425A1

    公开(公告)日:2024-07-11

    申请号:US18402153

    申请日:2024-01-02

    IPC分类号: C07C69/34 C07C69/63

    摘要: The invention relates to a process for preparing pilocarpine and intermediate compounds therefor. In particular, the present invention relates to key intermediates for the preparation of pilocarpine, i.e., compounds of formula I and formula II, and processes for their preparation. One method is to use malic acid as a raw material, react it with alcohol or sulfate ester first, then react with haloethane, etc. to obtain the compound of formula II, and finally react with a halogenating reagent to obtain the compound of formula I; in the other method, n-butyraldehyde is used as a raw material, and is subjected to condensation reaction, oxidation reaction, esterification reaction and sulfonylation reaction in sequence to obtain the compound of formula II, and finally react with a halogenating reagent to obtain the compound of formula I. The preparation method of the present invention has the advantages of mild reaction conditions, simple reaction process, high overall yield and high purity of the target product, and is therefore very suitable for industrial production.

    Solubization of resveratrol glycolate and tartrate derivatives

    公开(公告)号:US10851042B2

    公开(公告)日:2020-12-01

    申请号:US16899432

    申请日:2020-06-11

    IPC分类号: C07C69/70 C07C69/34

    摘要: A process for solubilizing a resveratrol glycolate compound by heating the resveratrol glycolate and mixing the resveratrol glycolate with one or more glycols is disclosed. The process comprises an initial heating step of the resveratrol compound to a temperature not greater than 45° C. and a mixing step that mixes the heated resveratrol glycolate compound with at least one glycol solvent at room temperature for ten minutes to one hundred and twenty minutes.

    Methods of sustaining dietary ketosis and its effects on lipid profile

    公开(公告)号:US10792268B2

    公开(公告)日:2020-10-06

    申请号:US15451891

    申请日:2017-03-07

    摘要: The ketogenic diet (KD) has therapeutic implications in many disease states. It was hypothesized ketone precursor supplementation would elevate blood ketone levels to therapeutic ranges (2-7 mM) without need for dietary restriction. The effects of ketogenic agents were tested on blood glucose, ketones, and lipids with a 28-day dose escalation study in male Sprague-Dawley rats: R,S-1,3-Butandiol (BD), acetoacetate ketone ester (KE), and control (H2O) (n≥8). Days 1-28, rats received a daily 5 g/kg intragastric gavage, based on previous toxicology studies. Once weekly, whole blood samples (10 μl) were acquired for analysis of glucose and βHB at 0, 0.5, 1, 4, 8, and 12 hours after test substance administration, or until βHB returned to baseline. At day 1 and 28, 10 μL of whole blood were collected to measure triglycerides, total cholesterol, and HDL concentration. Significant elevation of blood ketone was observed with a significant inverse relationship with blood glucose for the duration of the experiment. There were no significant changes in the lipid panel for any of the substances. There were significant reductions in body weight when animals were treated with either BD or KE as compared to control.