- Berbamine Analogs Exhibit Differential Protective Effects From Aminoglycoside-Induced Hair Cell Death
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Hearing loss is the third most common chronic health condition in the United States and largely results from damage to sensory hair cells. Major causes of hair cell damage include aging, noise exposure, and medications such as aminoglycoside antibiotics.
- Hudson, Alexandria M.,Lockard, Gavin M.,Namjoshi, Ojas A.,Wilson, Joseph W.,Kindt, Katie S.,Blough, Bruce E.,Coffin, Allison B.
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- Synthesis technology of higenamine and pharmaceutical salt of higenamine
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The invention discloses a synthesis technology of higenamine and pharmaceutical salt of the higenamine, and belongs to the technical field of medicine synthesis. According to the synthesis technology,4-methoxyphenylacetic acid is used as a raw material, and through steps of reduction, oxidation, cyclization, deprotection and the like, the higenamine and the hydrochloride of the higenamine are obtained. Compared with existing technical routes, the synthesis technology has the few steps, and is simple to operate, the raw material is cheap, reaction conditions are mild, a reaction process is easy to control, the total yield and the purity are high, and the synthesis technology is environmentally friendly, safe and suitable for industrial production, and has large industrial prospects.
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Paragraph 0055-0056
(2019/09/14)
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- Tetrahydroisoquinoline derivative and application thereof
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Provided are a tetrahydroisoquinoline derivative and an application thereof. The invention relates to a compound represented by the formula (V) and a preparation method and an application thereof in medicines. In particular, the invention relates to the d
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Paragraph 0226; 0227; 0229
(2016/10/09)
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- Enantioselective Oxidative Aerobic Dealkylation of N-Ethyl Benzylisoquinolines by Employing the Berberine Bridge Enzyme
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N-Dealkylation methods are well described for organic chemistry and the reaction is known in nature and drug metabolism; however, to our knowledge, enantioselective N-dealkylation has not been yet reported. In this study, exclusively the (S)-enantiomers o
- Gandomkar, Somayyeh,Fischereder, Eva-Maria,Schrittwieser, Joerg H.,Wallner, Silvia,Habibi, Zohreh,Macheroux, Peter,Kroutil, Wolfgang
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p. 15051 - 15054
(2016/01/25)
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- Synthesis of (+)-O-methylthalibrine by employing a stereocontrolled Bischler-Napieralski reaction and an electrochemically generated diaryl ether
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An efficient electrochemical four-step route was developed for the preparation of diaryl ether derivatives by using halogenation and dehalogenation processes in addition to electrochemical phenolic oxidation and reduction reactions. The synthesis of (+)-O
- Kawabata, Yuki,Naito, Yu,Saitoh, Tsuyoshi,Kawa, Kohei,Fuchigami, Toshio,Nishiyama, Shigeru
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- Synthesis and structure activity relationship of tetrahydroisoquinoline- based potentiators of GluN2C and GluN2D containing N-Methyl-D-aspartate receptors
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We describe here the synthesis and evaluation of a series of tetrahydroisoquinolines that show subunit-selective potentiation of NMDA receptors containing the GluN2C or GluN2D subunits. Bischler-Napieralski conditions were employed in the key step for the
- Santangelo Freel, Rose M.,Ogden, Kevin K.,Strong, Katie L.,Khatri, Alpa,Chepiga, Kathryn M.,Jensen, Henrik S.,Traynelis, Stephen F.,Liotta, Dennis C.
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p. 5351 - 5381
(2013/07/26)
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- Synthesis of 8-oxoberbines and related benzolactams by Pd(OAc) 2-catalyzed direct aromatic carbonylation
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A variety of alkoxy-substituted benzolactams with a berbine or yohimbane skeleton were prepared from 1-benzyl-1,2,3,4-tetrahydroisoquinolines or 1-benzyl-1,2,3,4-tetrahydro-β-carbolines by a phosphine-free Pd(II)-catalyzed direct aromatic carbonylation in a Pd(OAc)2-Cu(OAc) 2 catalytic system. The site selectivity was compared with that of the carbonylation with Pd(OAc)2 or Pd(OAc)2·2 PPh3, respectively.
- Miyazawa, Mamoru,Tokuhashi, Takashi,Horibata, Akiyoshi,Nakamura, Takatoshi,Onozaki, Yu,Kurono, Nobuhito,Senboku, Hisanori,Tokuda, Masao,Ohkuma, Takeshi,Orito, Kazuhiko
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- Oxidation of 1-benzyldihydroisoquinolines or 1- benzyltetrahydroisoquinolines with dioxygen to 1-benzoylisoquinolines
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An environmental-benign methodology to synthesize 1-benzoylisoquinolines from 1-benzyl-3, 4-dihydroisoquinolines or 1-benzyl-1,2,3,4- tetrahydroisoquinolines using dioxygen as an oxidant was developed. This methodology in combination with Bischler-Napieralski reaction leads to a facile synthesis of 1-benzoylisoquinolines from phenylacetic acids and phenylethanamines.
- Gan, Haifeng,Lu, Yunyu,Huang, Yue,Ni, Lijun,Xu, Jinyi,Yao, Hequan,Wu, Xiaoming
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body text
p. 1320 - 1324
(2011/04/15)
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- Synthesis of tetrahydroisoquinoline alkaloids via anodic cyanation as the key step
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We report a new route to tetrahydroisoquinoline (THIQ) alkaloids involving the alkylation of α-aminonitrile 2 as a key step. The latter compound was prepared by anodic cyanation of the corresponding tertiary amine 1. Reductive decyanation of α-aminonitriles 6a-c proceeded diastereoselectively (up to 95% de) to deliver the C1-substituted alkaloids precursors 9a-c. The syntheses of (±)-carnegine, (±)-norlaudanosine, and (±)-O,O- dimethylcoclaurine have been achieved.
- Louafi, Fadila,Hurvois, Jean-Pierre,Chibani, Aissa,Roisnel, Thierry
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supporting information; experimental part
p. 5721 - 5724
(2010/11/04)
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- A new benzylisoquinoline alkaloid from Argemone mexicana
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A new benzylisoquinoline alkaloid, argemexirine, together with two known protoberberine alkaloids, dl-tetrahydrocoptisine and dihydrocoptisine, have been isolated from the methanolic extract of the whole plant of Argemone mexicana L. The compounds were identified by spectral and chemical evidence. This is the first report of these alkaloids in this plant species.
- Singh, Sarita,Singh,Singh,Pandey
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experimental part
p. 63 - 67
(2010/04/23)
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- Method and health food for preventing and/or alleviating psychiatric disorder, and/or for effectuating sedation
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A method for preventing and/or alleviating a psychiatric disorder, and/or effectuating sedation, comprising administering a benzylisoquinoline derivative represented by General Formula (I): wherein R1, R2, R3 and X each re
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Page/Page column 9
(2008/06/13)
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- Synthesis of (±)-Glaucine and (±)-Neospirodienone via an One-Pot Bischler-Napieralski Reaction and Oxidative Coupling by a Hypervalent Iodine Reagent
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Condensation of 3,4-dimethoxybenzeneethanamine (3d) and various benzeneacetic acids, i.e., 4a-e, via a practical and efficient one-pot Bischler-Napieralski reaction, followed by NaBH4 reduction, produced a series of 1-benzyl-1,2,3,4-tetrahydroisoquinolines, i.e., 5a-e, in satisfactory yields (Scheme 3). Oxidative coupling of the N-acyl and N-methyl derivatives 6a-e of the latter with hypervalent iodine ([IPh(CF 3COO)2]) yielded products with two different skeletons (Scheme 4). The major products from N-acyl derivatives 6a-c were (±)-N-acylneospirodienones 2a-c, while the minor was the 3,4-dihydroisoquinoline 7. (±)-Glaucine (1), however, was the major product starting from N-methyl derivative 6e. Possible reaction mechanisms for the formation of these two types of skeleton are proposed (Scheme 5).
- Huang, Wei-Jan,Singh, Om V.,Chen, Chung-Hsiung,Lee, Shoei-Sheng
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p. 167 - 174
(2007/10/03)
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- Simplified tetrandrine congeners as possible antihypertensive agents with a dual mechanism of action
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A series of O- and/or N-substituted derivatives of (±)-coclaurine (1a) were synthesized as simplified structural mimics of the antihypertensive alkaloid tetrandrine (2) and assayed for binding to brain cortical sites labeled with the α1-adrener
- Iturriaga-Vasquez, Patricio,Miquel, Raquel,Ivorra, M. Dolores,D'Ocon, M. Pilar,Cassels, Bruce K.
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p. 954 - 957
(2007/10/03)
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