The aromatic difluoromethyl group (Ar-CF₂H) is an emerging functional group found in pharmaceutical compoundsFor synthesis, the hydrodefluorination of Ar-CF₃ mols. is a straightforward approach in terms of atom economy and substrate scope.The reported hydrodefluorination reaction focused on the Ar-CF₃ substrate bearing electron-withdrawing groups.In this report, electricity was utilized as the driving force for the hydrodefluorination of ArCF₃, which involved electron-donating groups.By using ammonia as a traceless hydrogen and electron donor, the reaction could tolerate a variety of labile groups, including unprotected amine, pyrrole, furan, thioether and silyl group, without sacrificial anodes in undivided cells.In this work, tBuOLi was found to be an essential additive for achieving good reactivity and chemoselectivity.Several Ar-CF₂H pharmaceutical and intermediate products were synthesized via this approach.

2017-01-01·Biological & pharmaceutical bulletin4区 · 医学

Influence of Characteristics of Oily Vehicle on Skin Penetration of Ufenamate

4区 · 医学

Article

作者: Kira, Hitomi ; Watanabe, Yoshiteru ; Koizumi, Naoya ; Fujii, Makiko ; Hashizaki, Kaname ; Iino, Hayato ; Fujino, Manami ; Kohara, Shizuka ; Utoguchi, Naoki

Skin penetration amounts of a highly lipophilic drug, ufenamate, prepared in four oily vehicles, including white petrolatum (WP), liquid paraffin (LP), isopropyl myristate (IPM), and isocetyl stearate (ICS), were compared. Ufenamate was mixed in each vehicle at 5% and applied at a rate of 2 mg/cm² to intact, stripped, and delipidized Yucatan micropig skin. The amounts of ufenamate and IPM in the stratum corneum (SC), epidermis, and dermis were determined. The skin penetration amounts of ufenamate from liquid oils were significantly higher than those from WP; the amounts of ufenamate were in the order WP

2015-01-01·Biological & pharmaceutical bulletin4区 · 医学

Penetration of Ufenamate into Intact, Stripped, or Delipidized Skin Using Different Vehicles

4区 · 医学

Article

作者: Koizumi, Naoya ; Watanabe, Yoshiteru ; Fujii, Makiko ; Fujino, Manami ; Iino, Hayato

The purpose of this study was to clarify the effect of skin condition on skin penetration of the very high lipophilic drug, ufenamate (UF). UF was applied to stripped or delipidized skin using liquid paraffin (LP) or purified water containing polysorbate 80 at a dose of 2 µL/cm(2). We found that UF penetration into intact and stripped skin using a water vehicle was respectively 5 and 10 times higher than that using LP. UF is freely soluble in oil and insoluble in water; thus, activity in water is higher than that in LP. Therefore, it is useful to use a water-based vehicle for both intact sites and those with defective stratum corneum (SC). Conversely, we found that delipidization of SC decreased the penetration of UF significantly with both LP and water, and the amount measured in the epidermis was 1 µg/cm(2) with both vehicles. This indicates that UF is not suitable for so-called "dry skin." This study revealed clinically relevant differences in the penetration of UF into intact, stripped, or delipidized skin conditions.

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KEGG	Wiki	ATC	Drug Bank
D01823	乌芬那酯	M01AG03	-

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
急性湿疹	日本	Viatris Pharmaceutical GK	1983-02-01
慢性湿疹	日本	Viatris Pharmaceutical GK	1983-02-01
口周皮炎	日本	Viatris Pharmaceutical GK	1983-02-01
酒渣鼻样皮炎	日本	Viatris Pharmaceutical GK	1983-02-01
特应性皮炎	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
接触性皮炎	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
脂溢性皮炎	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
带状疱疹	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07
湿疹	日本	Mitsubishi Tanabe Pharma Corp.	1982-10-07