CAS: 136-95-8; Benzo[d]Thiazol-2-Amine

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94787-08-3 14779-17-0 2536-91-6

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CAS号333-20-0 硫氰酸钾 | CAS号2516-40-7 2-溴-1,3-苯并噻唑 | CAS号108-94-1 环己酮 | CAS号103-85-5 N-苯基硫脲 | CAS号615-20-3 2-氯苯并噻唑 | CAS号95-16-9 苯并噻唑 | CAS号137-07-5 2-氨基苯硫酚 | CAS号1032-98-0 3-(2-benzothiaz... | CAS号615-21-4 2-肼基苯并噻唑 | CAS号1141-88-4 2,2'-二氨基二苯二硫醚 | CAS号14294-12-3 (9CI)-2-苯并噻唑硫脲 | CAS号20415-66-1 1,3-benzothiazo... | CAS号17930-02-8 2-(4-氰基苯基)苯并噻唑 | CAS号21418-25-7 diethyl 2-[(1,3... | CAS号19412-20-5 N-(1,3-benzothi... | CAS号1849-86-1 1-benzothiazol-... | CAS号21786-97-0 4-氧-4H-苯并[D]嘧啶[...

苯并噻唑置于2,2,6,6-Tetramethylpiperidinylmagnesium Chloride Lithium Chloride Complex,(1R,4S)-1,3,3-Trimethylspiro[bicyclo[2.2.1]Heptane-2,3'-[1,2]Oxaziridine],氯化铵体系中,用 四氢呋喃,甲苯,水 用作溶剂,化学反应 2.0H,以26%的收率获得2-氨基苯并噻唑
参考文献:利用多功能试剂支架将杂原子快速转移至芳基金属
标题:利用多功能试剂支架将杂原子快速转移至芳基金属
摘要:芳基金属是非常有价值的碳亲核体,可以容易地和廉价地从芳基卤化物或芳烃制得,并且广泛用于实验室和工业规模以直接与各种亲电体反应.尽管cc键的形成一直是有机合成的主要内容,但是由于缺乏氨基,伯氨基(-Nh 2)和羟基(-Oh)以可扩展且对环境友好的方式直接转移至芳基金属仍然是一项艰巨的合成挑战.合适的杂原子转移试剂.在这里,我们演示了基准稳定的nh和n的使用衍生自易于获得的类萜骨架的-烷基恶唑烷,作为有效的多功能试剂,可用于结构多样的芳基和杂芳基金属的直接伯胺化和羟基化.这种实用且可扩展的方法可在低温下一步一步合成伯胺和苯酚,并且避免使用过渡金属催化剂,配体和添加剂,氮保护基,过量的试剂和苛刻的后处理条件.
Doi:10.1038/nchem.2672

专利信息

专利号:US-6251689-B1
优先权日:1998-05-14
标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof
发明人：LABORDE EDGARDO; MATSUMOTO YUKIHARU
权利人:TELIK INC
摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.

专利号:US-9512096-B2
优先权日:2011-12-22
标题 :Synthesis of amine substituted 4,5,6,7-tetrahydrobenzothiazole compounds
发明人：CHEN WEIRONG; HUMORA MICHAEL; KWOK DAW-LONG ALBERT; KIESMAN WILLIAM F; IRDAM ERWIN AYANDRA
权利人:KNOPP BIOSCIENCES LLC; KNOPP BIOSCIENCES LLP
摘要:The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.

专利号:US-2004101523-A1
优先权日:1989-07-27
标题:Renal-selective prodrugs for control of renal smpathetic nerve activity in the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-γ-glutamyl fusaric acid hydrazide (shown below) is preferred.

专利号:WO-9101724-A1
优先权日:1989-07-27
标题 :Renal-selective prodrugs for the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as depa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitors compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kidney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase inhibitors, of which N-acetyl-Y-glutamyl fusaric acid is preferred.

专利号:WO-9201667-A1
优先权日:1990-07-25
标题 :Renal-selective prodrugs for control of renal sympathetic nerve activity in the treatment of hypertension
发明人：REITZ DAVID B; KOEPKE JOHN P; BLAINE EDWARD H; SCHUH JOSEPH R; MANNING ROBERT E; SMITS GLENN J
权利人:SEARLE & CO
摘要:Renal-selective prodrugs are described which are preferentially converted in the kidney to compounds capable of inhibiting synthesis of catecholamine-type neurotransmitters involved in renal sympathetic nerve activity. The prodrugs described herein are derived from inhibitor compounds capable of inhibiting one or more of the enzymes involved in catecholamine synthesis, such compounds being classifiable as tyrosine hydroxylase inhibitors, or as dopa-decarboxylase inhibitors, or as dopamine-β-hydroxylase inhibitors. These inhibitor compounds are linked to a chemical moiety, such as a glutamic acid derivative, by a cleavable bond which is recognized selectively by enzymes located predominantly in the kydney. The liberated inhibitor compound is then available in the kidney to inhibit one or more of the enzymes involved in catecholamine synthesis. Inhibition of renal catecholamine synthesis can suppress heightened renal nerve activity associated with sodium-retention related disorders such as hypertension. Conjugates of particular interest are glutamyl derivatives of dopamine-β-hydroxylase-inhibitors, of which N-acetyl-η-glutamyl fusaric acid hydrazide [represented in formula (a)] is preferred.

专利号:US-2025129021-A1
优先权日:2023-09-19
标 题:Small molecule protein synthesis modulators
发明人：GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE
权利人:INTERDICT BIO INC
摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.