Nucleophilic Addition of Amides to Haloalkynes: Synthesis of (Z)-ß-Halovinyl Amides as Dual Precursors of Alkylidene Carbenes and Allyl Halides.

Toward a regioselective method for the synthesis of ß-halovinyl amides, we developed a transition-metal-free nucleophilic addition reaction of amides to haloalkynes. The regioselective nucleophilic addition was achieved under solvent-free conditions using phosphonates to protonate the intermediate alkylidene carbenoids, thus suppressing their decomposition. Furthermore, we demonstrate that ß-halovinyl amides can serve as dual precursors of allyl halides and alkylidene carbenes to obtain functionalized indoles and pyrrolidones.

One-minute mental status examination for category fluency is more useful than mini-mental state examination to evaluate the reliability of insulin self-injection in elderly diabetic patients.

AIMS/INTRODUCTION: We investigated the factors associated with the reliability of insulin self-injection in elderly diabetic patients receiving insulin therapy. MATERIALS AND METHODS: We enrolled diabetic patients aged ≥65 years and receiving insulin therapy, and assessed their cognitive function by the mini-mental state examination and 1-min mental status examination for category fluency. We also observed their technique of insulin self-injection, and evaluated whether or not patients were able to inject insulin by themselves according to nine defined details in terms of insulin self-injection. The predictive factors for the reliability of insulin self-injection were determined by univariate and multivariate logistic regression analysis. There were 278 participants (135 males, 143 females) enrolled in the present study. RESULTS: According to multivariate logistic regression analysis, only the 1-min mental status examination score was found to be a significant independent predictor of the reliability of insulin self-injection (odds ratio 0.75; 95% confidence interval 0.62-0.90; P = 0.002). CONCLUSIONS: The 1-min mental status examination for category fluency can be considered more useful than mini-mental state examination to evaluate the reliability of insulin self-injection in elderly diabetic patients receiving insulin therapy.

[A questionnaire survey on current status of anti-diabetic therapy for diabetic patients with dementia].

AIM: It is important to establish treatment goals and optimal anti-diabetic therapy for diabetic patients with dementia. However, there are currently no established treatment guidelines. Recently, the West Tokyo Diabetes Association has established the Diabetes and Dementia Study Group to investigate the status of anti-diabetic therapy for diabetic patients with dementia. Here, we assessed the current status of such patients by a questionnaire survey. METHODS: In November 2011, we conducted a mailed survey to the clinics and hospitals affiliated with Kita-Tama, Hachioji and Tachikawa Medical Associations in Tokyo, Japan. The survey evaluated the most suitable anti-diabetic therapy for elderly diabetic patients or diabetic patients with dementia, combined anti-diabetic therapy, insulin therapy for elderly diabetic patients and diabetic patients with dementia, combination therapy of insulin and oral anti-diabetic agents for diabetic patients with dementia, factors that make it difficult for diabetic patients with dementia to continue insulin therapy, and selection of treatment or care for diabetic patients with dementia. RESULTS: The responses indicated that the anti-diabetic agents appropriate for diabetic patients with dementia are dipeptidyl peptidase-4 inhibitors. Those inappropriate for the same patients are metformin and insulin. Family support was a major factor for insulin therapy continuation for diabetic patients with dementia. Moreover, anti-diabetic agents for these patients are selected according to their ease of use and compatibility with available familial and social resources. CONCLUSION: Our survey results can be utilized for the creation of new guidelines and educational resources for the anti-diabetic therapy of diabetic patients with dementia.

Preparation of L-vancosamine-related glycosyl donors.

An improved practical synthesis of L-vancosamine-related glycosyl donors is described. The key steps include (1) stereoselective addition of methylcerium reagent to oximino ether and (2) stereoselective hydrogenation of exocyclic unsaturated glycoside in the presence of Wilkinson catalyst with C(5) inversion to give L-vancosamine derivatives. Three glycosyl donors were prepared, and their reactivities in the aryl C-glycoside formation were compared. Conversion of primary amine and azide to the corresponding N,N-dimethyl derivative is also described.

Selective formation of twisted intramolecular charge transfer and excimer emissions on 2,7-bis(4-diethylaminophenyl)-fluorenone by choice of solvent.

We designed and synthesized a donor-acceptor-donor dye consisting of a 2,7-disubstituted fluorenone with diethylaminophenyl moieties present as strong electron donating groups. Switching between twisted intramolecular charge transfer (TICT) emission and excimer emission was achieved, with no ground state changes, by simply changing the solvent used. In a nonpolar solvent, excimer emission was observed; with increasing polarity, the emission gradually disappeared, and the TICT emission appeared.