+++ Синтез 4-[1-(4-метилинданил)]-1H-имидазола
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pashkaru
+++ Синтез 4-[1-(4-метилинданил)]-1H-имидазола
Помогите пожалуста, кто чем может: советом или ссылкой...Заранее спасибо!
Последний раз редактировалось pashkaru Чт июл 14, 2011 6:27 pm, всего редактировалось 5 раз.
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pashkaru
Re: Синтез производных имидазола
Предложили сварить метилинданон и 4-иодимидазол и сшить их через Гриньяра. Но беда в том, что с Гриньяром не доводилось работать. Как инданон сделать нашел, а в остальном проблемы 
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suprachemister
- Сообщения: 4884
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Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
look in this references:
1. Pharmacophore model analysis of medetomidine and its analogs
By Ding, Xiao-qin; Yang, Ju-hui; Zhao, Li-feng; Shao, Hua-zhou; Luo, Qing-chong
From Jisuanji Yu Yingyong Huaxue (2002), 19(1/2), 19-24. Language: Chinese, Database: CAPLUS
4-Substituted imidazole analogs is a new class of selective α2-adrenoceptor agonists. Medetomidine is its representative and is used as a veterinary sedative-anesthetic drug. In this paper three-dimensional pharmacophore models of this series compd. binding to α1 and α2-adrenoceptor have been studied using Catalyst software. The correlate coeff. of the two models are 0.96 and 0.99 resp. and shows good predictive ability. Based on the pharmacophore model, a 3D-QSAR anal. was performed and can guide us to design new selective α2-adrenoceptor agonists.
2. Medetomidine Analogs as α2-Adrenergic Ligands. 3. Synthesis and Biological Evaluation of a New Series of Medetomidine Analogs and Their Potential Binding Interactions with α2-Adrenoceptors Involving a "Methyl Pocket"
By Zhang, Xiaoyan; De Los Angeles, Joseph E.; He, Mei-Ying; Dalton, James T.; Shams, Gamal; Lei, Longping; Patil, Popat N.; Feller, Dennis R.; Miller, Duane D.; Hsu, Fu-Lian
From Journal of Medicinal Chemistry (1997), 40(19), 3014-3024. Language: English, Database: CAPLUS
The synthesis and the biol. evaluation of a new series of medetomidine analogs are reported. The substitution pattern at the Ph ring of the tetralin analogs had a distinct influence on the α2-adrenoceptor binding affinity. 4-[1-(4-Methylindanyl)]-1H-imidazole was the most potent α2-adrenoceptor binding ligand among these 4-substituted imidazoles, and its α2-adrenoceptor selectivity was greater than the 5-Me tetralin analog, 4-(5-methyl-1,2,3,4-tetrahydro-1-naphthyl)-1H-imidazole. Ligand-pharmacophore and receptor modeling were combined to rationalize α2-adrenoceptor binding data of the imid...
3. Biological evaluation of a new series of medetomidine analogs and molecular basis for the binding of medetomidine analogs to α2-adrenoceptors
By Miller, D. D.; De Los Angeles, J.; Dalton, J. T.; He, M.-Y.; Zhang, X.; Shams, G.; Lei, L.; Patil, P. N.; Feller, D. R.; Hsu, F. L.
Edited by Berg, Dorothy A
From Proceedings of the ERDEC Scientific Conference on Chemical and Biological Defense Research, Aberdeen Proving Ground, Md., Nov. 14-17, 1995 (1996), 1047-1052. Language: English, Database: CAPLUS
The biol. evaluation of a new series of medetomidine analogs are reported. In the tetralin series, substituents on the Ph ring seem to have an important influence on α2-binding affinity. The 5-Me tetralin analog and the 4-Me indan analog were found to be the most potent α1-antagonists of the imidazole series and had excellent inhibitory activity at human platelet aggregation. We used an approach in which ligand-pharmacophore and homol.-based receptor modeling are combined to rationalize α2-adrenergic binding data of the imidazole analogs in terms of ligand-receptor interactions. The struct...
4. Preparation of indanylimidazole derivatives and related compounds having affinity for α2 receptors.
By Karjalainen, Arto; Huhtala, Paavo; Savola, Juha-Matti; Wurster, Siegfried; Eloranta, Maire; Savola, Maarit; Saxlund, Raimo; Cockcroft, Victor; Karjalainen, Arja
From PCT Int. Appl. (1997), WO 9712874 A1 19970410. Language: English, Database: CAPLUS
Title compds. [I; n = 0, 1; R1, R3, R5, R9, R10 = H, alkyl; R2 = H; R2R3 = bond; R4 = H, OH, alkyl, alkoxy; R4R5C = carbonyl group; R6, R7, R8 = H, OH, SH, alkyl, alkenyl, cycloalkyl, alkoxy, hydroxyalkyl, alkylthio, alkylthiol, halo, CF3, NO2, (substituted) amino; X = CHR9(CHR10)m; m = 0, 1], were prepd. Use of I for treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction, anxiety, neurol., musculoskeletal, psychiatric and cognition disorders and as adjuncts to anesthesia, is claimed. Thus, 1-(3-benzyl-3H-imidazol-4-yl)ethanone and 1-...
1. Pharmacophore model analysis of medetomidine and its analogs
By Ding, Xiao-qin; Yang, Ju-hui; Zhao, Li-feng; Shao, Hua-zhou; Luo, Qing-chong
From Jisuanji Yu Yingyong Huaxue (2002), 19(1/2), 19-24. Language: Chinese, Database: CAPLUS
4-Substituted imidazole analogs is a new class of selective α2-adrenoceptor agonists. Medetomidine is its representative and is used as a veterinary sedative-anesthetic drug. In this paper three-dimensional pharmacophore models of this series compd. binding to α1 and α2-adrenoceptor have been studied using Catalyst software. The correlate coeff. of the two models are 0.96 and 0.99 resp. and shows good predictive ability. Based on the pharmacophore model, a 3D-QSAR anal. was performed and can guide us to design new selective α2-adrenoceptor agonists.
2. Medetomidine Analogs as α2-Adrenergic Ligands. 3. Synthesis and Biological Evaluation of a New Series of Medetomidine Analogs and Their Potential Binding Interactions with α2-Adrenoceptors Involving a "Methyl Pocket"
By Zhang, Xiaoyan; De Los Angeles, Joseph E.; He, Mei-Ying; Dalton, James T.; Shams, Gamal; Lei, Longping; Patil, Popat N.; Feller, Dennis R.; Miller, Duane D.; Hsu, Fu-Lian
From Journal of Medicinal Chemistry (1997), 40(19), 3014-3024. Language: English, Database: CAPLUS
The synthesis and the biol. evaluation of a new series of medetomidine analogs are reported. The substitution pattern at the Ph ring of the tetralin analogs had a distinct influence on the α2-adrenoceptor binding affinity. 4-[1-(4-Methylindanyl)]-1H-imidazole was the most potent α2-adrenoceptor binding ligand among these 4-substituted imidazoles, and its α2-adrenoceptor selectivity was greater than the 5-Me tetralin analog, 4-(5-methyl-1,2,3,4-tetrahydro-1-naphthyl)-1H-imidazole. Ligand-pharmacophore and receptor modeling were combined to rationalize α2-adrenoceptor binding data of the imid...
3. Biological evaluation of a new series of medetomidine analogs and molecular basis for the binding of medetomidine analogs to α2-adrenoceptors
By Miller, D. D.; De Los Angeles, J.; Dalton, J. T.; He, M.-Y.; Zhang, X.; Shams, G.; Lei, L.; Patil, P. N.; Feller, D. R.; Hsu, F. L.
Edited by Berg, Dorothy A
From Proceedings of the ERDEC Scientific Conference on Chemical and Biological Defense Research, Aberdeen Proving Ground, Md., Nov. 14-17, 1995 (1996), 1047-1052. Language: English, Database: CAPLUS
The biol. evaluation of a new series of medetomidine analogs are reported. In the tetralin series, substituents on the Ph ring seem to have an important influence on α2-binding affinity. The 5-Me tetralin analog and the 4-Me indan analog were found to be the most potent α1-antagonists of the imidazole series and had excellent inhibitory activity at human platelet aggregation. We used an approach in which ligand-pharmacophore and homol.-based receptor modeling are combined to rationalize α2-adrenergic binding data of the imidazole analogs in terms of ligand-receptor interactions. The struct...
4. Preparation of indanylimidazole derivatives and related compounds having affinity for α2 receptors.
By Karjalainen, Arto; Huhtala, Paavo; Savola, Juha-Matti; Wurster, Siegfried; Eloranta, Maire; Savola, Maarit; Saxlund, Raimo; Cockcroft, Victor; Karjalainen, Arja
From PCT Int. Appl. (1997), WO 9712874 A1 19970410. Language: English, Database: CAPLUS
Title compds. [I; n = 0, 1; R1, R3, R5, R9, R10 = H, alkyl; R2 = H; R2R3 = bond; R4 = H, OH, alkyl, alkoxy; R4R5C = carbonyl group; R6, R7, R8 = H, OH, SH, alkyl, alkenyl, cycloalkyl, alkoxy, hydroxyalkyl, alkylthio, alkylthiol, halo, CF3, NO2, (substituted) amino; X = CHR9(CHR10)m; m = 0, 1], were prepd. Use of I for treatment of hypertension, glaucoma, chronic or acute pain, migraine, diarrhea, common cold, ischemia, addiction, anxiety, neurol., musculoskeletal, psychiatric and cognition disorders and as adjuncts to anesthesia, is claimed. Thus, 1-(3-benzyl-3H-imidazol-4-yl)ethanone and 1-...
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pashkaru
Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
Ну и оперативность!!!!!!!!! 
Круто!!! Спасибо огромное, будем разбераться...
Круто!!! Спасибо огромное, будем разбераться...-
pashkaru
Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
Блин, не могу найти первые три ссылки!!! Патенты нашел, а остальное все через платные базы данных предлагается! Можно выложить ссылки на свободный ресурс????? С телефона особо не полазишь по инету...
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suprachemister
- Сообщения: 4884
- Зарегистрирован: Пн май 18, 2009 5:34 pm
Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
2
У вас нет необходимых прав для просмотра вложений в этом сообщении.
Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
А я уйду из бытия, в небытиё, оно мое.
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pashkaru
Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
Во! То что надо!!! Спасибо, Великий Гуру!suprachemister писал(а):2
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suprachemister
- Сообщения: 4884
- Зарегистрирован: Пн май 18, 2009 5:34 pm
Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
1
У вас нет необходимых прав для просмотра вложений в этом сообщении.
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pashkaru
Re: Синтез 4-[1-(4-метилинданил)]-1H-имидазол
Тут ток справочная информация, но все одно спасибо!!!suprachemister писал(а):1
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