Syntheses of (±)-2-[(Inden-7-yloxy) methyl] morpholine Hydrochloride (YM-08054,Indeloxazine Hydrochloride) and Its Derivatives with Potential Cerebral-Activating and Antidepressive Properties

スポンサーリンク

概要

• 論文の詳細を見る

• The synthesis of (±)-2-[(inden-7-yloxy) methyl] morpholine hydrochloride (7・HCl, YM-08054,indeloxazine hydrochloride) and its optical resolution into levo- and dextro-isomers were investigated. A practical synthetic method for 7・HCl was established by employing preferential crystallization from an equilibrium mixture of 7・HCl and its tautomer, (±)-2-[(inden-4-yloxy)-methyl] morpholine hydrochloride (6・HCl), in the presence of a catalytic amount of base in MeOH. It was found that 7・HCl and its levo-rotatory isomer ((-)-7・HCl) showed not only strong antidepressive activities, but also potent cerebral-activating properties. The syntheses and pharmacological activities of related compounds are also discussed briefly.

• 社団法人日本薬学会の論文
• 1985-09-25

著者

• 藤倉 峻

  山之内製薬

• 小嶋 淳男

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 新形 邦宏

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 藤倉 峻

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 立川 四郎

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 野崎 順久

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 加賀美 壮一

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 高橋 孝三

  Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd.

• 野崎 順久

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 藤倉 峻

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 新形 邦宏

  山之内製薬株式会社創薬研究本部

• 高橋 孝三

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 新形 邦宏

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 立川 四郎

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 小嶋 淳男

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

• 加賀美 壮一

  Central Research Laboratories Yamanouchi Pharmaceutical Co. Ltd.

関連論文

• DMAB誘発ラット前立腺癌の発癌予防に関する研究
• Syntheses of (±)-2-[(Inden-7-yloxy) methyl] morpholine Hydrochloride (YM-08054,Indeloxazine Hydrochloride) and Its Derivatives with Potential Cerebral-Activating and Antidepressive Properties
• Synthesis of 2-N, N-Dialkylamino-1-aroyloxybenzocycloalkanes
• Studies on Antitumor Substances. V. Reaction of Thiosulfonates with Active Methylene Compounds.
• Synthesis of New Water-soluble Dihydropyridine Vasodilators
• Absolute Configurations of Four Isomers of 3-Formamido-4-hydroxy-α-[[N-(p-methoxy-α-methylphenethyl) amino] methyl] benzyl Alcohol, a Potent β-Adrenoreceptor Stimulant
• New β-Adrenoreceptor Stimulants. Studies on 3-Acylamino-4-hydroxy-α-(N-substituted aminomethyl) benzyl Alcohols
• 含硫黄ピリミド[5,4-d]ピリミジン化合物の合成研究(第4報)4,8-Dipiperidino-pyrimido[5,4-d]pyrimidine-2,6-disulfonyl Dichlorideとジエタノールアミンの反応によるDipyridamoleの生成機構
• Unambiguous Synthesis of 1-(7-Indenyloxy)-3-isopropylamino-2-propanol Hydrochloride and Its 4-Indenyloxy Isomer, Potent β-Adrenergic Blocking Agents
• Lactol Esters of Ampicillin
• 排尿障害治療薬タムスロシンの発見と開発研究
• アドレナリン受容体遮断薬とキラリティー : α, βおよびα・β遮断薬を例として
• DMAB誘発ラット前立腺発癌に対するAromatase inhibitorの効果
• 新規α_1受容体遮断薬, 塩酸タムスロシンの研究開発
• Synthesis, Resolution, and Renal Vasodilation Activity of Novel DA_1 Agonists : 4-(3,4-Dihydroxyphenyl)-1,2,3,4-tetrahydroisoquinoline Derivatives
• インデン環を有する新しいβ-受容体遮断剤の合成
• Studies on Benzenesulfonamide Derivatives with α-and β-Adrenergic Antagonistic and Antihypertensive Activities
• Studies on Antitumor Substances. III. Syntheses of Bis(methanesulphonylthio)alkanes
• STUDIES ON THE REACTION OF THIAMINE WITH PHOSGENE

もっと見る 閉じる

スポンサーリンク