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

Paroxetine CAS Registry Number: 61869-08-7 帕罗西汀

CAS Name: (3S-trans)-3-[(1,3-Benzodioxol-5-yloxy)methyl]-4-(4-fluorophenyl)piperidine
Additional Names: (-)-trans-4-(p-fluorophenyl)-3-[[3,4-(methylenedioxy)phenoxy]methyl]piperidinePercent Com...
Literature References: Selective serotonin (5-HT) reuptake inhibitor (SSRI). Prepn: J. A. Christensen, R. F. Squires, DE 2404113; eidem, US 3912743; US 4007196 (1974, 1975, 1977 all to Ferrosan); of crystalline hydrochloride hemihydrate: R. D. B. Barnes et al., EP 223403; US 4721723 (1987, 1988 both to Beecham). Characterization of serotonin inhibition: J. Buus Lassen, Eur. J. Pharmacol. 47, 351 (1978). Binding to serotonin transporter complex: E. Habert et al., ibid. 118, 107 (1985). Clinical pharmacokinetics: J. Lund et al., Acta Pharmacol. Toxicol. 51, 351 (1982). HPLC determn in plasma: M. A. Brett et al., J. Chromatogr. 419, 438 (1987). Clinical trial in obsessive-compulsive disorder: J. Zohar et al., Br. J. Psychiatry 169, 468 (1996); in social phobia: M. B. Stein et al., J. Am. Med. Assoc. 280, 708 (1998). Review of pharmacology and clinical use in depression: K. L. Dechant, S. P. Clissold, Drugs 41, 225-253 (1991); of clinical experience: D. Dunner, R. Kumar, Pharmacopsychiatry 31, 89-101 (1998); of use in generalized social anxiety disorder: M. Van Ameringen et al., Expert Opin. Pharmacother. 6, 819-830 (2005).

Ritanserin CAS Registry Number: 87051-43-2 利坦丝林

CAS Name: 6-[2-[4-[Bis(4-fluorophenyl)methylene]-1-piperidinyl]ethyl]-7-methyl-5H-thiazolo[3,2-a]pyrimidin-5-oneTrademarks: Tiserton (Janssen)
Percent Composition: C 67.90%, H 5.28%, F 7.96%, N...
Literature References: Selective serotonin (5-HT2) receptor antagonist. Prepn: L. E. J. Kennis et al., EP 110435; eidem, US 4533665 (1984, 1985 both to Janssen). Pharmacological profile: F. Awouters et al., Drug Dev. Res. 15, 61 (1988). GC/MS determn in plasma and pharmacokinetics: P. Timmerman et al, Biomed. Environ. Mass Spectrom. 18, 498 (1989). Clinical studies: G. Nappi et al., Headache 30, 439 (1990); G. Bersani et al., Acta Psychiatr. Scand. 83, 244 (1991); J. M. Monti et al., Sleep 16, 647 (1993).

Eltoprazine CAS Registry Number: 98224-03-4 依托拉嗪

CAS Name: 1-(2,3-Dihydro-1,4-benzodioxin-5-yl)piperazine
Additional Names: 1-(1,4-benzodioxan-5-yl)piperazine
Percent Composition: C 65.43%, H 7.32%, N 12.72%, O 14.53%
Literature References: Selective serotonin 5HT1 agonist; psychotropic agent with antiagressive activity. Prepn: J. Hartog et al., EP 138280; idem et al., EP 189612 (1985, 1986 both to Duphar). Prepd (not claimed): idem et al., US 4833142 (1989 to Duphar). Crystal structure: M. L. Verdonk et al., Acta Crystallogr. C48, 2271 (1992). Series of articles on pharmacology, receptor binding and mechanism of action: Drug Metab. Drug Interact. 8, 1-186 (1990). Pharmacokinetics: M. H. de Vries et al., Eur. J. Clin. Pharmacol. 41, 485 (1991). Clinical evaluation in self-injury: W. M. A. Verhoeven et al., Lancet 340, 1037 (1992); in violent psychiatric patients: J. Tiihonen et al., ibid. 341, 307 (1993).

Lesopitron CAS Registry Number: 132449-46-8 来索吡琼

CAS Name: 2-[4-[4-(4-Chloro-1H-pyrazol-1-yl)butyl]-1-piperazinyl]pyrimidine
Percent Composition: C 56.16%, H 6.60%, Cl 11.05%, N 26.20%
Literature References: Selective serotonin 5HT1A-receptor agonist. Prepn: A. Colombo Pinol et al., EP 382637; eidem, US 5128343 (1990, 1992 both to Esteve). Receptor binding studies and pharmacology: B. Costall et al., J. Pharmacol. Exp. Ther. 262, 90 (1992); M. Ballarin et al., Br. J. Pharmacol. 113, 425 (1994). Gastroprotective effects: A. J. Farré et al., J. Pharmacol. Exp. Ther. 272, 832 (1995).

Rizatriptan CAS Registry Number: 144034-80-0 利扎曲坦

CAS Name: N,N-Dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole-3-ethanamine
Additional Names: 3-[2-(dimethylamino)ethyl]-5-(1H-1,2,4-triazol-1-ylmethyl)indole; N,N-dimethyl-2-[5-(1,2,4-triazo...
Literature References: Selective serotonin 5-HT1D receptor agonist; structurally derived from tryptamine. Prepn: R. Baker et al., EP 497512; eidem, US 5298520 (1992, 1994 both to Merck Sharp Dohme); and binding characteristics: L. J. Street et al., J. Med. Chem. 38, 1799 (1995). Synthesis: C. Chen et al., Tetrahedron Lett. 35, 6981 (1994). Clinical pharmacokinetics: H. Cheng et al., Biopharm. Drug Dispos. 17, 17 (1996). LC-MS determn in plasma: D. A. McLoughlin et al., J. Chromatogr. A 726, 115 (1996). Comparative clinical trial in treatment of migraine: J. U. Adelman et al., Neurology 57, 1377 (2001). Review of pharmacology and therapeutic efficacy: K. Wellington, G. L. Plosker, Drugs 62, 1539-1574 (2002).

Nefazodone CAS Registry Number: 83366-66-9 奈法唑酮

CAS Name: 2-[3-[4-(3-Chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-2,4-dihydro-4-(2-phenoxyethyl)-3H-1,2,4-triazol-3-one
Additional Names: 2-[3-[4-(3-chlorophenyl)-1-piperazinyl]propyl]-5-ethyl-4...
Literature References: Selective serotonin 5-HT2 receptor antagonist. Prepn: D. L. Temple, Jr., W. G. Lobeck, Jr., US 4338317 (1982 to Mead Johnson). Synthesis and x-ray crystal structure: G. D. Madding et al, J. Heterocycl. Chem. 22, 1121 (1985). Pharmacology: A. S. Eison et al., Psychopharmacol. Bull. 26, 311 (1990). HPLC determn in plasma: J. E. Franc et al., J. Chromatogr. 570, 129 (1991). Clinical trial in depression: M. F. D'Amico et al., Psychopharmacol. Bull. 26, 147 (1990); in combination with psychotherapy for chronic depression: M. B. Keller et al., N. Engl. J. Med. 342, 1462 (2000). Review: W. E. Heydorn, Expert Opin. Invest. Drugs 4, 131-137 (1995).

Ramosetron CAS Registry Number: 132036-88-5 拉莫司琼

CAS Name: (1-Methyl-1H-indol-3-yl)[(5R)-4,5,6,7-tetrahydro-1H-benzimidazol-5-yl]methanone
Additional Names: (R)-5-[(1-methylindol-3-yl)carbonyl]-4,5,6,7-tetrahydrobenzimidazolePercent Compositi...
Literature References: Selective serotonin 5HT3 receptor antagonist; structurally different from ondansetron, granisetron, q.q.v. Prepn: M. Ohta et al., EP 381422; eidem, US 5344927 (1990, 1994 both to Yamanouchi). Pharmacology: K. Miyata et al., J. Pharmacol. Exp. Ther. 259, 15 (1991). Effects on gastric emptying in rodents: K. Miyata et al., Jpn. J. Pharmacol. 69, 205 (1995). Toxicity evaluation: H. Tabata et al., Arzneim.-Forsch. 45, 760 (1995). HPLC determn in plasma and urine: H. Miura et al., Biomed. Chromatogr. 8, 103 (1994). Clinical prevention of postoperative nausea and vomiting: Y. Fujii et al., Anesth. Analg. 90, 472 (2000).

Tegaserod CAS Registry Number: 145158-71-0 马来酸替加色罗

CAS Name: 2-[(5-Methoxy-1H-indol-3-yl)methylene]-N-pentylhydrazinecarboximidamide
Percent Composition: C 63.76%, H 7.69%, N 23.24%, O 5.31%
Literature References: Selective serotonin 5HT4-receptor partial agonist. Prepn: R. K. A. Giger, H. Mattes, EP 505322; eidem, US 5510353 (1992, 1996 both to Sandoz); K.-H. Buchheit et al., J. Med. Chem. 38, 2331 (1995). Clinical pharmacology: S. Appel et al., Clin. Pharmacol. Ther. 62, 546 (1997); and pharmacokinetics: idem et al., J. Clin. Pharmacol. 37, 229 (1997). Clinical trial in irritable bowel syndrome: S. A. Müller-Lissner et al., Aliment. Pharmacol. Ther. 15, 1655 (2001); in female patients: J. Novick et al., ibid. 16, 1877 (2002). Review of clinical efficacy: B. W. Jones et al., J. Clin. Pharm. Ther. 27, 343-352 (2002); of mechanism of action, efficacy and safety: M. Corsetti, J. Tack, Expert Opin. Pharmacother. 3, 1211-1218 (2002).

Fluvoxamine CAS Registry Number: 54739-18-3 氟伏沙明

CAS Name: (E)-5-Methoxy-1-[4-(trifluoromethyl)phenyl]-1-pentanone O-(2-aminoethyl)oxime
Additional Names: 5-methoxy-4'-(trifluoromethyl)valerophenone (E)-O-(2-aminoethyl)oxime
Percent Compos...
Literature References: Selective serotonin reuptake inhibitor (SSRI). Prepn: NL 7503310; H. B. A. Welle, V. Claassen, US 4085225 (1975, 1978 both to Philips-Duphar). Inhibition of 5-HT uptake: V. Claassen et al., Br. J. Pharmacol. 60, 505 (1977). HPLC determn in plasma: G. J. De Jong, J. Chromatogr. 183, 203 (1980). Series of articles on pharmacology, pharmacokinetics and clinical trials in depression: Br. J. Clin. Pharmacol. 15, Suppl. 3, 347S-450S (1983). Clinical trial in obsessive-compulsive disorder: L. M. Koran et al., J. Clin. Psychopharmacol. 16, 121 (1996). Review of clinical experience in depression: M. R. Ware, J. Clin. Psychiatry 58, Suppl. 5, 15-23 (1997).

Dapoxetine CAS Registry Number: 119356-77-3 达泊西汀

CAS Name: (aS)-N,N-Dimethyl-a-[2-(1-naphthalenyloxy)ethyl]benzenemethanamine
Additional Names: (+)-N,N-dimethyl-1-phenyl-3-(1-naphthalenyloxy)propanaminePercent Composition: C 82.59%, H 7.59%, ...
Literature References: Selective serotonin reuptake inhibitor (SSRI). Prepn: D. W. Robertson et al., EP 288188; eidem, US 5135947 (1988, 1992 both to Lilly). Chiral synthesis: W. J. Wheeler, D. D. O'Bannon, J. Labelled Compd. Radiopharm. 31, 305 (1992). HPLC determn in plasma: C. L. Hamilton, J. D. Cornpropst, J. Chromatogr. 612, 253 (1993). Review of pharmacology and clinical experience: B. Feret, Formulary 40, 227-230 (2005).