Enantioselective synthesis of hyperparathyroidism agent Cinacalcet hydrochloride

A simple and efficient route has been developed for enantioselective synthesis of hyperparathyroidism agent (R)-Cinacalcet. The synthesis started from commercially available triflouromethyl benzaldehyde and 1-(naphthalen-1-yl) ethanone and completed in 8 steps with an overall yield 18.5%. The key reactions involved are Corey-Bakshi-Shibata chiral reduction and reductive amination

Enantioselective synthesis of hyperparathyroidism agent Cinacalcet hydrochloride

503-507A simple and efficient route has been developed for enantioselective synthesis of hyperparathyroidism agent (R)-Cinacalcet. The synthesis started from commercially available triflouromethyl benzaldehyde and 1-(naphthalen-1-yl) ethanone and completed in 8 steps with an overall yield 18.5%. The key reactions involved are Corey-Bakshi-Shibata chiral reduction and reductive amination

Aza-Michael reactions in ionic liquids. A facile synthesis of β-amino compounds

Electron-deficient olefins undergo smoothly aza-Michael reactions with a wide range of amines in ionic liquids in the absence of any acid catalyst to produce the corresponding β-amino compounds in excellent yields with high 1,4-selectivity. The recovered ionic liquids can be reused in subsequent reactions without loss of activity. Owing to the high polarity of ionic liquids, the enones show enhanced reactivity thereby reducing reaction times and improving the yields significantly

Visual impairment among weaving communities in Prakasam district in South India.

PURPOSE: To assess the prevalence and causes of visual impairment in weaving communities in Prakasam district in South India state of Andhra Pradesh. METHODS: Using Rapid Assessment of Visual Impairment (RAVI) methodology, a population based cross-sectional study was conducted. A two-stage sampling strategy was used to select 3000 participants aged ≥40 years. Visual Acuity (VA) was assessed using a tumbling E chart and ocular examinations were performed by trained Para medical ophthalmic personnel. A questionnaire was used to collect personal and demographic information. Blindness and moderate Visual Impairment (VI) was defined as presenting VA <6/60 and <6/18 to 6/60 respectively. VI included blindness and moderate VI. RESULTS: 2848 of 3000 enumerated subjects (94.0%) participated. 39% were in 40-49 years age group and 11.8% were aged ≥70 years, 55% were women and nearly half of them had no formal education. 400 (14%; 95% CI: 12.8-15.3) subjects had VI, including blindness in 131 (4.6%; 95% CI: 3.8-5.4) and moderate VI in 269 (9.4%; 95% CI: 8.3-10.5) individuals. On applying multiple logistic regression, VI was significantly associated with older age and no formal education. Though the odds of having VI were higher in females, it was of borderline statistical significance (p = 0.06). Refractive error was the leading cause of all VI followed by cataract (56%). However, refractive errors were the leading cause of moderate VI (73.2%) and cataract was the leading cause of blindness (62.6%). 'Cannot afford the cost of services' was the leading barrier for utilization of eye care services (47%). CONCLUSIONS: There is a significant burden of VI in weaving communities in Andhra Pradesh, India most of which is avoidable. With this information as baseline, services need to be streamlined to address this burden

Three-component coupling reactions in ionic liquids: an improved protocol for the synthesis of 1,4-dihydropyridines

Three-component condensation of aldehyde, β-ketoester and methyl 3-aminocrotonate proceeds smoothly in 1-n-butyl-3-methylimidazolium tetrafluoroborate [bmim]BF<SUB>4</SUB> or 1-n-butyl-3-methylimidazolium hexafluorophosphate [bmim]PF<SUB>6</SUB> ionic liquids at room temperature under mild conditions to afford the corresponding 1,4-dihydropyridine derivatives in high yields. The recovered activated ionic liquids are recycled for four to five runs with no loss in activity

Baeyer-Villiger oxidations in ionic liquids. A facile conversion of ketones to esters and lactones

A variety of cyclic and acyclic ketones underwent readily oxidation with m-chloroperbenzoic acid (m-CPBA) in ionic liquid 1-butyl-3-methylimidazolium tetrafluoroborate [bmim]BF<SUB>4</SUB> to afford esters/lactones with high selectivity, ease of product separation and in excellent chemical yields. The reaction proceeded smoothly in ionic liquid without the need of any additional acid or base catalyst. The ketones show enhanced reactivity in ionic liquids thereby reducing reaction times and improving the yields significantly