The article confers a scalable manufacturing process of Fenspiride HCl. 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol is the main building block in Fenspiride HCl synthesis. The reported reagents for 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol synthesis are costly, explosive, highly toxic, produce hazardous waste, and also need to be handled with most care. The paper introduces aqueous ammonia as an alternate reagent in Fenspiride HCl and used in 4-aminomethyl-1-(2-phenylethyl)-piperidin-4-ol synthesis. The new green chemistry aspect makes the process environment-friendly and cheaper. It also eliminates toxic, sensitive, and hazardous reagents and makes the process safe on uncomplicated on bulk scale production. The high pure Fenspiride HCl is obtained by following this process and meets the ICH limits with good yield.
An improved and simplified process of vitamin K1 preparation. The article confers the new reagent BF3. Acetic acid complex as a condensation reagent for phytol with compound III in vitamin K1 synthesis, which eludes the use of ethereal reagent and make the process hazard free. Further innovation presents base catalyzed synthesis of vitamin K1 which is an oxidative product of compound IV. Sodium methoxide base is used in synthesis which eliminates use of metal oxidant, costly and hazardous reagent. The new approach ensures the non-generation of epoxide impurity (V) which tends to form during Ag2O catalyzed synthesis. Finally, article also focused on formation and conformation of 7R and 11R diastereomeric centers and ensure the formation of vitamin k1 with desired stereochemistry also article submit proof of concept and supporting literature survey for desired stereochemistry.
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