CAS: 33286-22-5; (2S,3S)-5-(2-(Dimethylamino)Ethyl)-2-(4-Methoxyphenyl)-4-Oxo-2,3,4,5-Tetrahydrobenzo[b][1,4]Thiazepin-3-Yl Acetate Hydrochloride

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CAS号42399-40-6 去乙酰地尔硫卓 | CAS号108-24-7 乙酸酐 | CAS号75472-91-2 DESACETYL DILTI... | CAS号108-22-5 醋酸异丙烯酯 | CAS号42399-48-4 (2S,3S)-threo-2... | CAS号2419-67-2 1-(4-Methoxyphe... | CAS号123-11-5 4-甲氧基苯甲醛; 对甲氧基苯... | CAS号42399-41-7 地尔硫卓 | CAS号42399-40-6 去乙酰地尔硫卓

(2S-Cis)-(+)-2,3-二氢-3-羟基-2-(4-甲氧苯基)-1,5-苯并硫氮杂卓-4(5H)-酮置于盐酸,Sodium Hydride体系中,用 乙醚,乙醇,N,N-二甲基甲酰胺,丁酮,Paraffin 作为反应溶剂,化学反应 4.0H,反应生成 盐酸地尔硫卓
参考文献:(2 S,3 S)-3-乙酰氧基-5-(二甲基氨基乙基)-2-(4-甲氧基苯基)-2,3-二氢-1,5-苯并噻嗪-4(5 H)-的绝对构型和构型氯化物(盐酸地尔硫卓)
标题:(2 S,3 S)-3-乙酰氧基-5-(二甲基氨基乙基)-2-(4-甲氧基苯基)-2,3-二氢-1,5-苯并噻嗪-4(5 H)-的绝对构型和构型氯化物(盐酸地尔硫卓)
摘要:通过辛可尼定盐3和brucine盐4拆分外消旋顺式-3-(2-氨基苯硫基)-2-羟基-3-(4-甲氧基苯基)丙酸(2),分离钙盐(+)-和描述了(-)-5以及它们对对映体1,5-苯并噻氮杂((+)-和(-)-1的环化.x射线单晶分析揭示了(+)-1的(2 S,3 S)绝对构型,是根据cd数据与已知的1,4-苯并二氮杂pine衍生物(+)-8的cd数据的初步比较得出的.配置.
DOI:10.1002/hlca.19840670333

专利信息

专利号:US-2022356139-A1
优先权日:2019-09-03
标 题:Synthesis of deuterated aldehydes
发明人：WANG WEI
权利人:ARIZONA BOARD OF REGENTS ON BEHALF OF ATHE UNIV OF ARIZONA
摘要:Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D 2 O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.

专利号:US-2023234932-A1
优先权日:2021-06-08
标 题:Synthesis and application of diltiazem hydrochloride
发明人：PAN SHUHUA; WANG JINYU; WANG SHOUCHUN
权利人:HAINAN JIN RUI PHARMACEUTICAL CO LTD
摘要:The invention belongs to the field of drug synthesis, the invention discloses a synthetic method and application of diltiazem hydrochloride. The synthesis method is through the condensation ring closing and esterification of cis-(2S,3S) compound 1 and compound 2, then add hydrochloric acid to form salt, get the diltiazem hydrochloride. The invention has the following advantages, shortens the synthesis steps, improves the reaction yield, reduces the industrial production cost, and saves the time cost of the synthesis. The method is used for the synthesis of diltiazem hydrochloride, and the synthesized diltiazem hydrochloride is used to prepare diltiazem hydrochloride for injection.

专利号:US-5302741-A
优先权日:1992-07-21
标 题:Optical resolution of threo-2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)-propionic acid
发明人：LIDOR RAMY; SINGER CLAUDE
权利人:TEVA PHARMA
摘要:D(+)-threo-2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, an important intermediate in the synthesis of diltiazem hydrochloride, is obtained in better yields and high optical purity by a novel resolution process comprising the reaction of 2 moles of the (±) racemic acid with 1 mole of quinine and 1 mole of a base in a suitable polar solvent system to form a salt of the D(+) acid and quinine which precipitates; separating said salt and decomposing it with a strong base.

专利号:EP-0415384-B1
优先权日:1989-08-31
标题 :Heterogeneous synthesis of azepinones from esters
发明人：MARTIN DANIEL E
权利人:HOECHST MARION ROUSSEL INC
摘要:An amino-acid ester compound can be cyclized into a cyclic amido-carbonyl compound by contacting the amino-acid ester compound in a liquid medium with a heterogeneous acidic ion-exchange substance. For example, 2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, methyl ester, threo form, can be cyclized in an aqueous mixture into cis-2-(4-methoxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H) -one by employing a sulfonated polystyrene-divinylbenzene ion-exchange resin in its acid form, e.g., Dowex 50X4-400, at yields exceeding 85 percent of theory, and the product can be used to make diltiazem hydrochloride.

专利号:US-5250680-A
优先权日:1989-08-31
标题:Heterogeneous synthesis of azepinones from esters
发明人：MARTIN DANIEL E
权利人:MERRELL DOW PHARMA
摘要:An amino-acid ester compound can be cyclized into a cyclic amido-carbonyl compound by contacting the amino-acid ester compound in a liquid medium with a heterogeneous acidic ion-exchange substance. For example, 2-hydroxy-3-(2-aminophenylthio)-3-(4-methoxyphenyl)propionic acid, methyl ester, threo form, can be cyclized in an aqueous mixture into cis-2-(4-methoxyphenyl)-3-hydroxy-2,3-dihydro-1,5-benzothiazepin-4(5H)-one by employing a sulfonated polystyrene-divinylbenzene ion-exchange resin in its acid form, e.g., Dowex® 50X4-400. at yields exceeding 85 percent of theory, and the product can be used to make diltiazem hydrochloride.

专利号:US-6187756-B1
优先权日:1996-09-05
标 题 :Composition and methods for treatment of neurological disorders and neurodegenerative diseases
发明人：LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , forskolin, or nicotine ditartrate is inhibited by immunosuppressants or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.