Abstract
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.
Highlights
Vitamin K plays a vital role in coagulation, bone development, and cardiovascular health
We started our work by following reported process [2,3] and we got required compound (I) and developed a commercially viable, sturdy process, which would be applicable to different analogues in the vitamin K family, especially keeping in view the most active compound, vitamin K1
The invention describes the improved synthesis of vitamin K1, which introduce new approach for the acylation reaction and avoids the usage of controlled substance like acetic anhydride
Summary
Vitamin K plays a vital role in coagulation, bone development, and cardiovascular health. Belmont and et al [4] discloses the reaction of 2methyl-1, 4-naphthohydroquinone with phytol or phytadiene in the temperature range of 70-1800C wherein oxalic acid and trichloroacetic acid are used as condensation agents and the reaction takes about twenty four hours for completion These described processes of vitamin K1 (I) preparation poses serious drawbacks especially for a commercial scale application. There still exists a need for an industrially viable and simplified process for synthesis of vitamin K1 (I) which avoids the use of hazardous reagent and solvents
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