Regioselective Synthesis of Trisubstituted Quinoxalines Mediated by Hypervalent Iodine Reagents.

A facile and regioselective synthesis of quinoxalines, an important motif in medicinal chemistry and materials sciences, was developed. Despite their prospective utility, the regioselective preparation of trisubstituted quinoxalines has not been previously established. In the reported system, hypervalent iodine reagents catalyzed the annulation between α-iminoethanones and o-phenylenediamines in a chemo/regioselective manner to afford trisubstituted quinoxalines. Excellent regioselectivities (6:1 to 1:0) were achieved using [bis(trifluoroacetoxy)iodo]benzene and [bis(trifluoroacetoxy)iodo]pentafluorobenzene as annulation catalysts.

Isolation, Structural Elucidation, and Anti-HIV Activity of Daphnane Diterpenoids from Daphne odora.

Five new [daphneodorins D-H (1, 5, and 10-12)] and seven known daphnane diterpenoids (2-4 and 6-9) were isolated from Daphne odora. The structures of the new compounds were elucidated by extensive physicochemical and spectroscopic analysis. The isolated compounds were evaluated for their anti-HIV activity against HIV-1 infection of MT4 cells. Nine daphnane diterpenoid orthoesters (1-9) showed potent anti-HIV activity with EC50 values of 1.5-7.7 nM.

[Evaluation of the relapse prevention program for substance abusers called "TAMARPP" at mental health and welfare center].

We developed the TAMA mental health and welfare center Relapse Prevention Program (TAMARPP) and evaluated the efficacy of the program. We provided the program for 59 substance abusers at Tokyo Tama Comprehensive Mental Health and Welfare Center, and conducted brief interviews and questionnaire surveys to them four times during eight months follow-up period. The main results were as follows. 1) Most of the subjects were before "hitting bottom". 2) More than half of the subjects continued participating in the program for more than 2 months and their attendance rate was fairly high. 3) Some of the subjects began joining a self-help group as N.A. and A.A. during the follow up period. 4) The mood states of the subjects were gradually improved during the period. 5) About one-third of the subjects abused substance again after two-month' program, but all of them continued to attend the program or a private counseling. Most of their families also continued having support from the center. These findings suggested it was meaningful to have such a friendly and less confrontational program as TAMARPP at our center to provide support for many substance abusers before "hitting bottom" and their families.

[Qualitative evaluation of TAMARPP, the relapse prevention program for substance abusers at the Mental Health and Welfare Center].

The development of an effective treatment system for patients with addiction-related problems like substance abuse or pathological gambling is urgently needed. The purpose of this study was to clarify the therapeutic factors of the Tama Mental Health and Welfare Center Relapse Prevention Program (TAMARPP). The program is provided at the Tama Comprehensive Center for Mental Health and Welfare, which is operated publicly by the Tokyo Metropolitan Government. Seven personnel (3 clinical psychologists, 2 public health nurses, and 2 recovering counselors) searched the consultation records of 31 participants who had continued treatment longer than 1 year, and made a list of qualitative factors that may positively impact participant outcome. The following six factors were extracted: 1) a "no-blame" atmosphere that makes participants feel safe and free; 2) a mutual helping process that enables participants to empathize with one another; 3) an individual-centered approach that focuses on a participant's motivation to recover; 4) a psycho-educational process that establishes treatment goals; 5) a treatment goal that involves some type of social role; and 6) the referral of graduates to another long-term treatment program such as Narcotics Anonymous. Our results suggest the need of personnel to provide treatment as follows: 1) keep the circumstances safe; 2) use a method that matches the participant's motivation; 3) refer graduates to another in-depth treatment program; 4) emphasize the relationship between thinking, emotion, and behavior; and 5) improve the quality of life of the participant. The missions of our center, an official institution that runs such a program, are as follows: 1) to be the first place at which addicts seek aid during the early stage; 2) to cooperate with other facilities in order to provide social resources that support recovery; and 3) to support patients suffering from both addiction and comorbid psychiatric diseases.