其它产品项目整合

项目整合的本质是一项集合成方法学、反应工程学与过程分析技术于一体的系统工程。其核心逻辑可以概括为以下几点：源头优选：利用如N-硝胺化学等底层方法学突破，从分子层面颠覆传统高成本、高污染路线。过程强化：依托连续流技术，攻克有机金属试剂应用、光化学反应放大等“不可能”任务，实现高危工艺的本质安全。系统集成：整合“反应-淬灭-分离”全流程，利用微流控与在线分析技术，消除批次间的差异，实现药品制造的连续化与智能化。当前，中间体工艺研发正在经历从“经验驱动”向“数据驱动”的转变。AI辅助路线设计、自动化高通量筛选与连续制造平台的结合，将使得“分子结构与最优工艺路径”之间的映射关系逐渐清晰。未来的竞争优势，将属于那些能够将底层化学创新与先进工程技术进行无缝整合的研发体系。
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其它产品项目整合

Quinapril CAS Registry Number: 85441-61-8 喹那普利

CAS Name: (3S)-2-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,2,3,4-tetrahydro-3-isoquinolinecarboxylic acid
Additional Names: (S)-2-[(S)-N-[(S)-1-carboxy-3-phenylprop...
Literature References: Angiotensin converting enzyme (ACE) inhibitor. Prepn: M. L. Hoefle, S. Klutchko, EP 49605; eidem, US 4344949 (both 1982 to Warner-Lambert); S. Klutchko et al., J. Med. Chem. 29, 1953 (1986). Synthesis of purified crystalline form: O. P. Goel, U. Krolls, US 4761479 (1988 to Warner-Lambert). Pharmacology: H. R. Kaplan et al., Fed. Proc. 43, 1326 (1984); M. J. Ryan et al., ibid. 1330. HPLC determn of quinapril and quinaprilat in plasma and urine: H. Hengy, M. Most, J. Liq. Chromatogr. 11, 517 (1988). Toxicity data: H. R. Kaplan et al., Angiology 40, 335 (1989). Review of pharmacology, pharmacokinetics and clinical experience in congestive heart failure and hypertension: C. R. Culy, B. Jarvis, Drugs 62, 339-385 (2002).

Imidapril CAS Registry Number: 89371-37-9 咪达普利

CAS Name: (4S)-3-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1-methyl-2-oxo-4-imidazolidinecarboxylic acid
Additional Names: (4S)-3-[(2S)-2-[N-[(1S)-1-(ethoxycarbonyl)-...
Literature References: Angiotensin converting enzyme (ACE) inhibitor. Prepn: N. Yoneda et al., EP 95163; eidem, US 4508727 (1983, 1985 both to Tanabe Seiyaku); K. Hayashi et al., J. Med. Chem. 32, 289 (1989). Series of articles on pharmacology, pharmacokinetics and metabolism in animals: Arzneim.-Forsch. 42, 446-512 (1992). HPLC determn in plasma and urine: K. Tagawa et al., J. Chromatogr. 617, 95 (1993). Clinical pharmacology: P. Démolis et al., Fundam. Clin. Pharmacol. 8, 80 (1994). Clinical trial in hypertension: M. J. Vandenburg et al., Br. J. Clin. Pharmacol. 37, 265 (1994).

Ramipril CAS Registry Number: 87333-19-5 雷米普利

CAS Name: [2S,3aS,6aS]-1-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]octahydrocyclopenta[b]pyrrole-2-carboxylic acid
Additional Names: N-(1S-carboethoxy-3-phenylpropyl)-...
Literature References: Angiotensin converting enzyme (ACE) inhibitor; converted to active, diacid metabolite, ramiprilat. Prepn: V. Teetz et al, EP 79022 (1983 to Hoechst A.G.), C.A. 100, 52012h (1984); E. H. Gold et al., US 4587258 (1986 to Schering Corp.); V. Teetz et al., Arzneim.-Forsch. 34, 1399 (1984). Radioimmunoassay determn in human serum and plasma: H. G. Eckert et al., ibid. 35, 1251 (1985). Toxicology: H. H. Donaubauer, D. Mayer, ibid. 38, 14 (1988). Symposium on pharmacology and clinical efficacy: Am. J. Cardiol. 59, 1D-177D (1987). Clinical trial in chronic nephropathy: P. Ruggenenti et al., Lancet 352, 1252 (1998). Clinical prevention of cardiovascular events in high-risk patients: HOPE Study Investigators, N. Engl. J. Med. 342, 145 (2000). Clinical trial in prevention of stroke: J. Bosch et al., Br. Med. J. 324, 1 (2002).

Moexipril CAS Registry Number: 103775-10-6 莫西卜里

CAS Name: (3S)-2-[(2S)-2-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]-1-oxopropyl]-1,2,3,4-tetrahydro-6,7-dimethoxy-3-isoquinolinecarboxylic acidPercent Composition: C 65.04%, H 6.87%, N 5.62%,...
Literature References: Angiotensin converting enzyme (ACE) inhibitor; dimethoxy analog of quinapril, q.v. Prepn: M. L. Hoefle, S. Klutchko, EP 49605; eidem, US 4344949 (both 1982 to Warner-Lambert); S. Klutchko et al., J. Med. Chem. 29, 1953 (1986). Pharmacology: O. Edling et al., J. Pharmacol. Exp. Ther. 275, 854 (1995). GC-MS determn in plasma: W. Hammes et al., J. Chromatogr. B 670, 81 (1995). Clinical trials in hypertension: W. B. White et al., J. Hum. Hypertens. 8, 917 (1994); M. Stimpel et al., Cardiology 87, 313 (1996).

Olmesartan CAS Registry Number: 144689-63-4 奥美沙坦酯

CAS Name: 4-(1-Hydroxy-1-methylethyl)-2-propyl-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester
Additional Names...
Literature References: Angiotensin II receptor antagonist. Prepn: H. Yanagisawa et al., EP 503785; eidem, US 5616599 (1992, 1997 both to Sankyo); eidem, J. Med. Chem. 39, 323 (1996). Clinical evaluation in hypertension: K. Püchler et al., J. Hypertens. 15, 1809 (1997). Review: M. Elisaf, Curr. Opin. Cardiovasc. Pulm. Renal Invest. Drugs 2, 378-383 (2000).

Telmisartan CAS Registry Number: 144701-48-4 替米沙坦

CAS Name: 4'-[(1,4'-Dimethyl-2'-propyl[2,6'-bi-1H-benzimidazol]-1'-yl)methyl][1,1'-biphenyl]-2-carboxylic acid
Additional Names: 4'-[[4-methyl-6-(1-methyl-2-benzimidazolyl)-2-propyl-1-benzimida...
Literature References: Angiotensin II receptor antagonist. Prepn: N. Hauel et al., EP 502314 (1992 to Thomae), C.A. 117, 251352 (1992); U. J. Ries et al., J. Med. Chem. 36, 4040 (1993). Pharmacology: W. Wienen et al., Br. J. Pharmacol. 110, 245 (1993). Binding study: W. Wienen, M. Entzeroth, J. Hypertens. 12, 119 (1994). Clinical pharmacology, pharmacokinetics: J. M. Neutel, D. H. G. Smith, Adv. Ther. 15, 206 (1998). Clinical trial in hypertension: D. H. G. Smith et al., ibid. 229. Review of pharmacology and clinical efficacy: K. J. McClellan, A. Markham, Drugs 56, 1039-1044 (1998).

Irbesartan CAS Registry Number: 138402-11-6 厄贝沙坦

CAS Name: 2-Butyl-3-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1,3-diazaspiro[4.4]non-1-en-4-one
Additional Names: 2-butyl-3-[p-(o-1H-tetrazol-5-ylphenyl)benzyl]-1,3-diazaspiro[4.4]non...
Literature References: Angiotensin II type 1 (AII1)-receptor antagonist. Prepn: C. Bernhart et al., WO 9114679; eidem, US 5270317 (1991, 1993 both to Sanofi); eidem et al., J. Med. Chem. 36, 3371 (1993). HPLC determn in plasma and urine: S.-Y. Chang et al., J. Chromatogr. B 702, 149 (1997). Metabolism: T. J. Chando et al., Drug Metab. Dispos. 26, 408 (1998). Review of pharmacology and clinical efficacy: J. C. Gillis, A. Markham, Drugs 54, 885-902 (1997). Renoprotective effect in diabetic nephropathy: E. J. Lewis et al., N. Engl. J. Med. 345, 851 (2001); H.-H. Parving et al., ibid. 870.

Candesartan CAS Registry Number: 139481-59-7 坎地沙坦

CAS Name: 2-Ethoxy-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-benzimidazole-7-carboxylic acid
Additional Names: 2-ethoxy-1-[4-[2-(1H-tetrazol-5-yl)phenyl]benzyl]-7-benzimidazoleca...
Literature References: Angiotensin II type-1 receptor antagonist. Prepn: T. Naka et al., EP 459136; eidem, US 5196444 (1991, 1993 both to Takeda); K. Kubo et al., J. Med. Chem. 36, 2182, 2343 (1993). Pharmacology: Y. Shibouta et al., J. Pharmacol. Exp. Ther. 266, 114 (1993). Clinical pharmacology, pharmacokinetics: T. Ogihara et al., Clin. Ther. 16, 74 (1994). Pilot study of cilexetil ester in essential hypertension: idem et al., ibid. 15, 684 (1993). Series of clinical trials in chronic heart failure: Lancet 362, 759-781 (2003).

Temocapril CAS Registry Number: 111902-57-9 替莫普利

CAS Name: (2S,6R)-6-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]tetrahydro-5-oxo-2-(2-thienyl)-1,4-thiazepine-4(5H)-acetic acid
Additional Names: (+)-(2S,6R)-6-[[(1S)-1-carboxy-3-phenylpropy...
Literature References: Angiotensin-converting enzyme (ACE) inhibitor. Hydrolyzed in vivo to the active diacid metabolite. Prepn: H. Yanagisawa et al., EP 161801; eidem, US 4699905 (1985, 1987 both to Sankyo); idem et al., J. Med. Chem. 30, 1984 (1987). Pharmacology: K. Oizumi et al., Jpn. J. Pharmacol. 48, 349 (1988). GC/MS determn in human plasma and urine: H. Shioya et al., J. Chromatogr. 496, 129 (1989). Clinical evaluation: M. Arita et al., Clin. Exp. Pharmacol. Physiol. 21, 195 (1994); and pharmacokinetics: S. Tokunaga et al., Drug Invest. 7, 161 (1994). Review: H. Koike et al., Annu. Rep. Sankyo Res. Lab. 44, 1-81 (1992).

Alacepril CAS Registry Number: 74258-86-9 阿拉普利

CAS Name: 1-[(2S)-3-(Acetylthio)-2-methyl-1-oxopropyl]-L-prolyl-L-phenylalanine
Additional Names: 1-(D-3-acetylthio-2-methylpropanoyl)-L-prolyl-L-phenylalanine; N-[1-[(S)-3-mercapto-2-methylpro...
Literature References: Angiotensin-converting enzyme (ACE) inhibitor. Prepn: T. Sawayama et al., JP Kokai 80 9058; eidem, US 4248883 (1980, 1981 both to Dainippon Pharm.). Pharmacology in animals: K. Takeyama et al., Arzneim.-Forsch. 35, 1502 (1985); eidem, ibid. 1507. Series of articles on pharmacology, metabolism, enzyme inhibiting activity: ibid. 36, 47-83 (1986). Metabolism to captopril, q.v.: K. Matsumoto et al., ibid. 40. HPLC determn of metabolites in plasma and urine: K. Hayashi et al., J. Chromatogr. 338, 161 (1985). Pharmacokinetics in humans: K. Onoyama et al., Clin. Pharmacol. 38, 462 (1985). Preclinical evaluation in essential hypertension: K. Mizuno et al., Res. Commun. Chem. Pathol. Pharmacol. 49, 175 (1985); H. Shionoiri et al., Curr. Ther. Res. 38, 537 (1985). Series of articles on toxicology: M. Iida et al., Yakuri to Chiryo 13, 7033-7121 (1985), C.A. 104, 21888h-21890c; 105, 396v (1986).