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

Flesinoxan CAS Registry Number: 98206-10-1 氟辛克生

CAS Name: N-[2-[4-[(2R)-2,3-Dihydro-2-(hydroxymethyl)-1,4-benzodioxin-5-yl]-1-piperazinyl]ethyl]-4-fluorobenzamide
Additional Names: (+)-(S)-p-fluoro-N-[2-[4-[2-(hydroxymethyl)-1,4-benzodioxan-...
Literature References: Serotonin (5-HT1A)-receptor agonist; phenylpiperazine derivative. Prepn: J. Hartog et al., EP 138280; eidem, US 4833142 (1985, 1989 both to Duphar). Synthesis and resolution of enantiomers: M. D. Ennis, N. B. Ghazal, Tetrahedron Lett. 33, 6287 (1992). GC determn in plasma and urine: M. P. van Berkel et al., Methodol. Surv. Biochem. Anal. 18, 209 (1988). Pharmacology: J. Schipper et al., Hum. Psychopharmacol. 6, S53 (1991). Clinical evaluation in depression: P. Grof et al., Int. Clin. Psychopharmacol. 8, 167 (1993).

Perospirone CAS Registry Number: 150915-41-6 哌罗匹隆

CAS Name: (3aR,7aS)-rel-2-[4-[4-(1,2-Benzisothiazol-3-yl)-1-piperazinyl]butyl]hexahydro-1H-isoindole-1,3(2H)-dione
Additional Names: cis-N-[4-[4-(1,2-benzisothiazol-3-yl)-1-piperazinyl]butyl]-1...
Literature References: Serotonin (5-HT2) and dopamine (D2) antagonist (SDA). Prepn (stereochem unspec): K. Ishizumi et al., EP 196096; eidem, US 4745117 (1986, 1988 both to Sumitomo). Prepn of cis-form: eidem, Chem. Pharm. Bull. 43, 2139 (1995). Receptor binding profile in rat brain: T. Kato et al., Jpn. J. Pharmacol. 54, 478 (1990). Pharmacology: H. Sakamoto et al., Pharmacol. Biochem. Behav. 60, 873 (1998). Clinical trial in schizophrenia: M. Murasaki et al., Clin. Eval. 24, 159 (1997). Review of pharmacological profile: Y. Ohno et al., Pol. J. Pharmacol. 49, 213-219 (1997); and clinical experience: S. V. Onrust, K. McClellan, CNS Drugs 15, 329-337 (2001).

Deramciclane CAS Registry Number: 120444-71-5 德伦环烷

CAS Name: N,N-Dimethyl-2-[[(1R,2S,4R)-1,7,7-trimethyl-2-phenylbicyclo[2.2.1]hept-2-yl]oxy]ethanamine
Additional Names: (-)-[1R,2S,4R]-2-(2-dimethylaminoethoxy)-2-phenyl-1,7,7-trimethylbicyclo[2...
Literature References: Serotonin (5-HT2)-receptor antagonist. Prepn: BE 886579; Z. Budai et al., US 4342762 (1981, 1982 both to Egyt); L. Ladanyi et al., Chirality 11, 689 (1999). LC/MS/MS determn in plasma: A. Tolokán et al., J. Chromatogr. A 896, 279 (2000). Receptor binding profile and pharmacology: I. Gacsalyi et al., Drug Dev. Res. 40, 333 (1997). Clinical pharmacokinetics and tolerability: H. Kanerva et al., Int. J. Clin. Pharmacol. Ther. 37, 589 (1999). Clinical evaluation in generalized anxiety disorder: H. Naukkarinen et al., Eur. Neuropsychopharmcol. 15, 617 (2005). Review: S. Koks, E. Vasar, Curr. Opin. Invest. Drugs 3, 289-294 (2002).

Itasetron CAS Registry Number: 123258-84-4 伊他司琼

CAS Name: 2,3-Dihydro-N-[(3-endo)-8-methyl-8-azabicyclo[3.2.1]oct-3-yl]-2-oxo-1H-benzimidazole-1-carboxamide
Additional Names: 2-oxo-N-1aH,5aH-tropan-3a-yl-1-benzimidazoline-1-carboxamide
Pe...
Literature References: Serotonin (5-HT3) receptor antagonist. Prepn: M. Turconi et al., EP 309423 (1989 to Istituto De Angeli); eidem, US 5223511 (1993 to Boehringer, Ing.); M. Turconi et al., J. Med. Chem. 33, 2101 (1990). Pharmacology: idem et al., Eur. J. Pharmacol. 203, 203 (1991). Mode of action: M. B. Passani et al., Br. J. Pharmacol. 112, 695 (1994). Clinical efficacy and tolerability: H. Goldschmidt et al., Anti-Cancer Drugs 8, 436 (1997). Review of therapeutic potential: M. B. Passani, R. Corradetti, CNS Drug Reviews 2, 195-213 (1996).

Xaliproden CAS Registry Number: 135354-02-8 扎利罗登

CAS Name: 1,2,3,6-Tetrahydro-1-[2-(2-naphthalenyl)ethyl]-4-[3-(trifluoromethyl)phenyl]pyridine
Percent Composition: C 75.57%, H 5.81%, F 14.94%, N 3.67%
Literature References: Serotonin 5HT1A-receptor agonist; enhances production of neurotrophic factors and extends motor neuron survival. Prepn: D. Nisato et al., EP 101381; eidem, US 4521428 (1984, 1985 both to Sanofi); of radiolabelled compound: N. Robic, J.-P. Noël, J. Labelled Compd. Radiopharm. 42, 109 (1999). Pharmacology and receptor binding: L. Cervo et al., Eur. J. Pharmacol. 253, 139 (1994). Effect on neuron survival: Y. Iwasaki et al., J. Neurol. Sci. 160, Suppl. 1, S92 (1998). Neuroprotective effect in animal model of multiple sclerosis: B. Bourrié et al., Proc. Natl. Acad. Sci. USA 96, 12855 (1999). Review of pharmacology and clinical potential in treatment of amyotrophic lateral sclerosis: J. Fournier et al., CNS Drug Rev. 3, 148-167 (1997).

Naratriptan CAS Registry Number: 121679-13-8 那拉曲坦

CAS Name: N-Methyl-3-(1-methyl-4-piperidinyl)-1H-indole-5-ethanesulfonamide
Percent Composition: C 60.87%, H 7.51%, N 12.53%, O 9.54%, S 9.56%
Literature References: Serotonin 5-HT1B/1D receptor agonist. Prepn: A. W. Oxford et al., EP 303507; eidem, US 4997841 (1989, 1991 both to Glaxo). Pharmacology and receptor binding study: H. E. Connor et al., Cephalalgia 17, 145 (1997). Determn in plasma and pharmacokinetics in rabbits: B. D. Duléry et al., J. Pharm. Biomed. Anal. 15, 1009 (1997). Clinical trial in migraine: H. Havanka et al., Clin. Ther. 22, 970 (2000).

Frovatriptan CAS Registry Number: 158747-02-5 夫罗曲坦

CAS Name: (3R)-2,3,4,9-Tetrahydro-3-(methylamino)-1H-carbazole-6-carboxamide
Additional Names: 3-methylamino-6-carboxamido-1,2,3,4-tetrahydrocarbazolePercent Composition: C 69.11%, H 7.04%, N 1...
Literature References: Serotonin 5-HT1B/1D receptor agonist. Prepn: F. D. King et al., WO 9300086; eidem, US 5464864 (1993, 1995 both to SmithKline Beecham). Pharmacology: A. A. Parsons et al., J. Cardiovasc. Pharmacol. 30, 136 (1997). Series of articles on pharmacology, safety and clinical studies: Headache 42, Suppl. 2, S45-S99 (2002). Review of clinical experience in cluster headaches: H. C. Siow et al., Cephalalgia 24, 1045-1048 (2004); in acute migraine: N. Poolsup et al., J. Clin. Pharm. Ther. 30, 521-532 (2005).

Eletriptan CAS Registry Number: 143322-58-1 依来曲普坦

CAS Name: 3-[[(2R)-1-Methyl-2-pyrrolidinyl]methyl]-5-[2-(phenylsulfonyl)ethyl]-1H-indole
Additional Names: 5-[2-(benzenesulfonyl)ethyl]-3-(1-methylpyrrolidin-2(R)-ylmethyl)-1H-indolePercent Com...
Literature References: Serotonin 5-HT1B/1D receptor agonist. Prepn: J. E. Macor, M. J. Wythes, WO 9206973; eidem, US 5545644 (1992, 1996 both to Pfizer). Pharmacology: E. Willems et al., Arch. Pharmacol. 358, 212 (1998). Affinity and specificity of receptor binding: C. Napier et al., Eur. J. Pharmacol. 368, 259 (1999). Clinical trial in comparison with sumatriptan, q.v.: P. J. Goadsby et al., Neurology 54, 156 (2000). Review of pharmacokinetics, and clinical efficacy: A. Bardsley-Elliot, S. Noble, CNS Drugs 12, 325-333 (1999).

Almotriptan CAS Registry Number: 154323-57-6 阿莫曲坦

CAS Name: 1-[[[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]methyl]sulfonyl]pyrrolidine
Additional Names: 1-[[3-(2-dimethylaminoethyl)-5-indolyl]methanesulphonyl]pyrrolidinePercent Composition: C 6...
Literature References: Serotonin 5HT1B/1D-receptor agonist. Prepn: D. F. Forner et al., WO 9402460; eidem, US 5565447 (1994, 1996 both to Almirall). Clinical pharmacokinetics: J. C. Fleishaker et al., Clin. Pharmacol. Ther. 67, 498 (2000). Review of pharmacology: F. Kamali, Curr. Opin. Cent. Peripher. Nerv. Syst. Invest. Drugs 2, 197-202 (2000); of clinical studies: D. W. Dodick, Expert Opin. Pharmacother. 4, 1157-1163 (2003).

Zolmitriptan CAS Registry Number: 139264-17-8 佐米曲普坦

CAS Name: (4S)-4-[[3-[2-(Dimethylamino)ethyl]-1H-indol-5-yl]methyl]-2-oxazolidinone
Additional Names: (S)-N,N-dimethyl-2-[5-(2-oxo-1,3-oxazolidin-4-ylmethyl)-1H-indol-3-yl]ethylamineTrademarks:...
Literature References: Serotonin 5HT1D-receptor agonist. Prepn: A. D. Robertson et al., WO 9118897 (1991 to Wellcome Foundation); eidem, US 5466699 (1995 to Burroughs Wellcome). Structure-activity and receptor binding study: R. C. Glen et al., J. Med. Chem. 38, 3566 (1995). Pharmacology: P. J. Goadsby, L. Edvinsson, Headache 34, 394 (1994). Clinical pharmacokinetics: E. Seaber et al., Br. J. Clin. Pharmacol. 41, 141 (1996). Clinical trial in migraine: S. J. Tepper et al., Curr. Med. Res. Opin. 15, 254 (1999). Review of clinical experience and pharmacokinetics: M. Gawel, I. Worthington, Expert Opin. Pharmacother. 6, 1019-1024 (2005).