A convenient method for synthesis of 2R,3S and 2S,3S N-Boc phenylalanine
epoxides using readily available allylamine is described. Previous
methods employed multistep synthetic routes from l-phenyl
alanine that include use of m-chloroperbenzoic acid
(m-CPBA) and a chromatographic method for purification
of the desired diastereomers. Column purification could be eliminated
by bringing in much improvement in the existing process. The process
was further enhanced by replacing m-CPBA with oxone,
an ecofriendly reagent advantageous for commercial application. The
overall green process discussed involves the recovery and recycling
of enantiomers of chiral allyl amines and judicial separation of diastereomers
of the epoxides using simple economical methods.
3-Methoxy-5-nitrobenzaldehyde undergoes Knoevenagel reaction with malonic acid to give 3-methoxy-5-nitrocinnamic acid (I). Treatment of I with thionyl chloride yielded 3-chloro-5-methoxy-7-nitrobenzo[b]thiophene-2-carbonyl chloride (II) in 45 % yield. The reaction of II with 2-nitrophenol in benzene gave 2-nitrophenyl 3-chloro-5-methoxy- 7-nitrobenzo[b]thiophene-2-carboxylate (IIIa) in 65 % yield. Finally, dehydrochlorinative photocyclization of IIIa in acetone in the presence of the base triethylamine afforded 10-methoxy-4,8-dinitro-6H-benzothieno_2,3-c_chromen-6-one (IVa). Thus, a series of derivatives IVa-i were synthesized in excellent yields. The structures of the obtained products were characterized by IR and 1H-NMR spectroscopy, as well as elemental analysis. Their purity was ascertained by chromatographic analysis. All the compounds were tested for their antibacterial activity against S. aureus, E. coli, B. subtilis and S. typhosa.
Modern medical Science has offered many surgical procedures like open and closed haemorrhoidectomy, anal dilatation, Sphincterotomy etc for haemorrhoides and fissure in ano. These operative procedures are associated with unavoidable sequel of symptoms like Pain, Discharge and Inflammation etc. Role of analgesia is vital in the treatment of post-operative pain. The mode of analgesia depends on degree or level of pain which is a subjective criteria. Analgesics routinely used are NSAIDs, opioids and corticosteroids. Side effects includes like Gastritis, Gastrointestinal bleeding etc. Hence, Analgesia has to be supplemented with antacids or H2 Receptor Agonists. Here, quest for knowledge for an alternative treatment to analgesics starts. According to Sushrutacharya, these diseases like Arsha and Parikartika are termed as Chhedya, i.e., treatable by surgery and he has indicated Yashtimadhu Ghrita in Shastranipataja Vedana. Methodology- In present study, total 100 postoperative patients of haemorrhoids and fissure in ano, randomly allocated into two groups (50 in each group). In Group A (n = 50), Yashtimadhu Ghrita Gudapurana was done every day after sitz bath for 5 days. In Group B (n = 50), local application of lignocaine jelly every day after sitz bath for 5 days. Result- Yashtimadhu Ghrita as a local application is clinically as effective as lignocaine jelly in the management of post operative pain in patients of hemorrhoids and fissures in ano. Conclusion- it was concluded that Yashtimadhu Ghrita is helpful in the management of pain in the post operative patient of haemorrhoids and fissure in ano
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