| Project/Area Number |
11672115
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| Research Category |
Grant-in-Aid for Scientific Research (C)
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| Allocation Type | Single-year Grants |
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| Section | 一般 |
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| Research Field |
Chemical pharmacy
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| Research Institution | Showa Pharmaceutical University |
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Principal Investigator |
SANO Takehiro Showa Pharmaceutical Universit Professor, 薬学部, 教授 (00077520)
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| Co-Investigator(Kenkyū-buntansha) |
SAITOH Toshiaki Showa Pharmaceutical Universit Research Associate, 薬学部, 助手 (00286882)
HORIGUHI Yoshie Showa Pharmaceutical Universit Associate Professor, 薬学部, 助教授 (70190254)
戸田 潤 昭和薬科大学, 薬学部, 教授 (90188756)
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| Project Period (FY) |
1999 – 2000
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| Project Status |
Completed (Fiscal Year 2001)
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| Budget Amount *help |
¥2,000,000 (Direct Cost: ¥2,000,000)
Fiscal Year 2000: ¥500,000 (Direct Cost: ¥500,000)
Fiscal Year 1999: ¥1,500,000 (Direct Cost: ¥1,500,000)
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| Keywords | terahydroquinoline / parkinson's disease / pummerer reaction / 1,2,3,4-tetrahydroquinoline / benzoazepine / benzothiazine / tetrahydroisoquinoline / tetrahydroquinoline / trifluoroacetic anhydride / sulfoxide / synthesis |
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| Research Abstract |
In order to contribute to the development of biological study of tetrahydroisoquinolines, amines present in human brain, we have investigated the development of method synthesizing the tetrahydroisoquinolines and their analogs. Some tetrahydroisoquinolines are known to be a toxin which induces Parkinson's disease, while 1-methyl-1, 2, 3, 4-tetrahydroisoquinoline protects the parkinsonism induced by these toxins. The synthesis of these compounds was achieved by applying Pummerer-type reaction. The method consists in the nuceophilic substitution reaction of aromatic ring to the sulfoxide mediated carbocation, was discovered to be highly efficient and widely applicable for synthesizing the variously substituted nitrogen heterocycles, 1, 2, 3, 4-tetrhahydroisoquinoline and benzoazepines.
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