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

Remacemide CAS Registry Number: 128298-28-2 立马醋胺

CAS Name: 2-Amino-N-(1-methyl-1,2-diphenylethyl)acetamide
Percent Composition: C 76.09%, H 7.51%, N 10.44%, O 5.96%
Literature References: NMDA receptor antagonist. Prepn: R. C. Griffith, J. J. Napier, EP 279937 (1988 to Pennwalt); see also: eidem, US 5331007 (1994 to Fisons). Pharmacology, metabolism and pharmacokinetics: K. T. Muir, G. C. Palmer, Epilepsy Res. Suppl. 3, 147 (1991). HPLC determn in plasma: J. W. Flynn, J. E. O'Brien, J. Chromatogr. 583, 91 (1992). Mechanism of action study: S. Subramaniam et al., J. Pharmacol. Exp. Ther. 276, 161 (1996). Neuroprotective properties: G. C. Palmer et al., Ann. N.Y. Acad. Sci. 765, 236 (1995). Clinical evaluation in neuroprotection during cardiac surgery: J. E. Arrowsmith et al., Stroke 29, 2357 (1998); in Parkinson's disease: Parkinson Study Group, Neurology 56, 455 (2001). Review of mechanism of action and clinical applications: S. C. Schachter, D. Tarsy, Expert Opin. Invest. Drugs 9, 871-883 (2000).

Amantadine CAS Registry Number: 768-94-5 金刚烷胺

CAS Name: Tricyclo[3.3.1.13,7]decan-1-amine
Additional Names: 1-adamantanamine; 1-aminoadamantane; 1-aminodiamantane (obsolete); 1-aminotricyclo[3.3.1.13,7]decane
Percent Composition: C 79.4...
Literature References: NMDA-receptor antagonist; also active vs influenza A virus. Prepn: H. Stetter et al., Ber. 93, 226 (1960); W. Haaf, ibid. 97, 3234 (1964); P. Kovacic, P. D. Roskos, Tetrahedron Lett. 1968, 5833. Antiviral activity: W. L. Davies et al., Science 144, 862 (1964). GC determn in biological samples and pharmacodynamics: W. E. Bleidner et al., J. Pharmacol. Exp. Ther. 150, 484 (1965). Pharmacology and toxicology: V. G. Vernier et al., Toxicol. Appl. Pharmacol. 15, 642 (1969). Comprehensive description: J. Kirschbaum, Anal. Profiles Drug Subs. 12, 1-36 (1983). Review of use vs influenza A: R. L. Tominack, F. G. Hayden, Infect. Dis. Clin. North Am. 1, 459-478 (1987); of pharmacokinetics: F. Y. Aoki, D. S. Sitar, Clin. Pharmacokinet. 14, 35-51 (1988). Review of NMDA receptor binding and neuroprotective properties: J. Kornhuber et al., J. Neural Transm. 43, Suppl., 91-104 (1994). Series of articles on clinical experience in Parkinson's disease: ibid. 46, Suppl., 399-421 (1995).

Sodium Cellulose Phosphate CAS Registry Number: 9038-41-9

Additional Names: SCP
Trademarks: Calcibind (Mission Pharmacal); Calcisorb (3M Pharma)
Literature References: Non-absorbable ion exchange resin with high affinity for calcium ions. Prepn: G. P. Touey, US 2759924 (1956 to Eastman Kodak). Use in treatment of hypercalcemia: C. Y. C. Pak et al., J. Clin. Endocrinol. Metab. 28, 1828 (1968). Mechanism of action: C. Y. C. Pak, J. Clin. Pharmacol. 13, 15 (1973). Clinical pharmacology: idem, ibid. 19, 451 (1979). Use in treatment of calcium urolithiasis: U. Backman et al., J. Urol. 123, 9 (1980); C. Y. C. Pak, Invest. Urol. 19, 187 (1981).

Rifaximin CAS Registry Number: 80621-81-4 利福昔明

CAS Name: (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-25-(Acetyloxy)-5,6,21,23-tetrahydroxy-27-methoxy-2,4,11,16,20,22,24,26-octamethyl-2,7-(epoxypentadeca[1,11,13]trienimino)benzofuro[4,5-e]...
Literature References: Nonabsorbable semisynthetic rifamycin antibiotic. Prepn: BE 888895; E. Marchi, L. Montecchi, US 4341785 (1981, 1982 both to Alfa); E. Marchi et al., J. Med. Chem. 28, 960 (1985); and NMR study: M. Brufani et al., J. Antibiot. 37, 1611 (1984). X-ray crystal structure: idem et al., ibid. 1623. In vitro and in vivo antibacterial activity: A. P. Venturini, E. Marchi, Chemioterapia 5, 257 (1986). Toxicological study: G. Borelli, D. Bertoli, ibid. 263. Clinical trial in travelers' diarrhea: R. Steffen et al., Am. J. Gastroenterol. 98, 1073 (2003). Review of activity, pharmacokinetics and clinical experience in gastrointestinal infections: J. C. Gillis, R. N. Brogden, Drugs 49, 467-484 (1995); D. B. Huang, H. L. DuPont, J. Infection 50, 97-106 (2005).

Salsalate CAS Registry Number: 552-94-3 双水杨酸酯

CAS Name: 2-Hydroxybenzoic acid 2-carboxyphenyl ester
Additional Names: disalicylic acid; salicylic acid bimolecular ester; salicyloxysalicylic acid; salicylsalicylic acidTrademarks: Disalcid (...
Literature References: Nonacetylated aspirin analog. Prepn: DE 211403 and DE 214044 (1909, both to Boehringer, Mann.), Frdl. 9, 928 and C.A. 4, 368 (1910); W. Baker et al., J. Chem. Soc. 1951, 201. Metabolism: S. M. Dromgoole et al., J. Pharm. Sci. 73, 1657 (1984). Clinical evaluation in arthritis: T. C. McPherson, Clin. Ther. 6, 388 (1984). Mechanism of action studies: C. A. Divincenzo, F. R. Venezio, Curr. Ther. Res. 42, 720 (1987). HPLC determn in plasma and urine: L. I. Harrison et al., J. Pharm. Sci. 69, 1268 (1980). Review of chemistry, pharmacokinetics, safety and clinical efficacy: P. T. Singleton, Clin. Ther. 3, 80-102 (1980).

Nabumetone CAS Registry Number: 42924-53-8 萘丁美酮

CAS Name: 4-(6-Methoxy-2-naphthalenyl)-2-butanone
Additional Names: 4-(6-methoxy-2-naphthyl)-butan-2-oneTrademarks: Arthaxan (GSK); Balmox (GSK); Consolan (Novo); Nabuser (Geymonat); Relafen (G...
Literature References: Nonacidic, lipophillic prodrug; metabolized in vivo to 6-methoxy-2-naphthylacetic acid which inhibits prostaglandin synthesis. Prepn: A. W. Lake, C. J. Rose, DE 2442305; eidem, US 4061779 (1975, 1977 both to Beecham); A. C. Goudie et al., J. Med. Chem. 21, 1260 (1978). Pharmacology: E. A. Boyle et al., J. Pharm. Pharmacol. 34, 562 (1982); B. Nunn, P. D. Chamberlain, ibid. 576. Metabolism: R. E. Haddock et al., Xenobiotica 14, 327 (1984). HPLC determn in plasma: J. E. Ray, R. O. Day, J. Chromatogr. 336, 234 (1984). Symposia on pharmacology, pharmacokinetics and clinical efficacy: Int. Congr. Symp. Ser. - R. Soc. Med. 69, 1-215 (1985); J. Rheumatol. 19, Suppl. 36, 1-91 (1992). Review: S. L. Dahl, Ann. Pharmacother. 27, 456-463 (1993).

Trithiozine CAS Registry Number: 35619-65-9 舒美吗啉

CAS Name: 4-[Thioxo(3,4,5-trimethoxyphenyl)methyl]morpholine
Additional Names: 4-(3,4,5-trimethoxythiobenzoyl)morpholine; sulmetozine (rescinded INN); tritiozineTrademarks: Tresanil (ISF)
Pe...
Literature References: Non-anticholinergic gastric secretion inhibitor. Prepn: G. Pifferi, DE 2102246; idem, US 3862138 (1972, 1975 both to ISF). Synthesis and pharmacology: G. Pifferi et al., Chim. Ther. 8, 462 (1973). HPLC determn in plasma and urine: T. Crolla et al., J. Chromatogr. 222, 257 (1981). Clinical studies: M. Elakovic et al., J. Int. Med. Res. 8, 347 (1980); U. Marini et al., Clin. Ter. 92, 399 (1980). Evaluation of gastric acid suppression: K. Gibinski, Curr. Med. Res. Opin. 7, 516 (1981).

Prephenic Acid CAS Registry Number: 126-49-8 (1-羧基-4-羟-2,5-环己二烯基)代丙酮酸

CAS Name: 1-Carboxy-4-hydroxy-a-oxo-2,5-cyclohexadiene-1-propanoic acid
Additional Names: 1-carboxy-4-hydroxy-2,5-cyclohexadiene-1-pyruvic acid
Percent Composition: C 53.10%, H 4.46%, O 42.4...
Literature References: Non-aromatic biosynthetic intermediate that represents a secondary branch-point in the pathway from chorismic acid to phenylalanine and tyrosine, q.q.v., in many organisms. Isoln from cultures of mutant Escherichia coli: B. D. Davis, Science 118, 251 (1953). Characterized as cryst Ba salt: U. Weiss et al., ibid. 119, 774 (1954); R. L. Metzenberg, H. K. Mitchell, Arch. Biochem. Biophys. 64, 51 (1956). Structure: H. Plieninger, G. Keilich, Z. Naturforsch. 16b, 81 (1961). Synthetic approaches: H. Plieninger, Angew. Chem. Int. Ed. 1, 367 (1962). Total synthesis of disodium salt: S. Danishevsky, M. Hirama, J. Am. Chem. Soc. 99, 7740 (1977); S. Danishevsky et al., ibid. 101, 7013 (1979); W. Gramlich, H. Plieninger, Ber. 112, 1571 (1979). Review: U. Weiss, J. M. Edwards, The Biosynthesis of Aromatic Compounds (Wiley, New York, 1980) pp 144-184. See also shikimic acid.

Ipsapirone CAS Registry Number: 95847-70-4 伊沙匹隆

CAS Name: 2-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-1,2-benzisothiazolin-3(2H)-one 1,1-dioxide
Additional Names: isapirone
Percent Composition: C 56.84%, H 5.77%, N 17.44%, O 11.96%, S 7....
Literature References: Nonbenzodiazepine anxiolytic; 5-hydroxytryptamine (5-HT1) receptor agonist. Prepn: W. Dompert et al., DE 3321969; P.-R. Seidel et al., US 4818756 (1984, 1989 both to Troponwerke). Pharmacology and serotonin (5-HT1) receptor binding study: J. Traber et al., Brain Res. Bull. 12, 741 (1984). 5-HT1 specific binding activity: W. U. Dompert et al., Arch. Pharmacol. 328, 467 (1985); T. Glaser, J. Traber, ibid. 329, 211 (1985). Behavioral effects in mice: R. J. DeSouza et al., Br. J. Pharmacol. 89, 377 (1986). Neurophysiological effects in comparison with buspirone. M. J. Rowan, R. Anwyl, Eur. J. Pharmacol. 132, 93 (1987). HPLC determn in biological samples: G. Bianchi, S. Caccia, J. Chromatogr. 431, 477 (1988).

Buspirone CAS Registry Number: 36505-84-7 丁螺环酮

CAS Name: 8-[4-[4-(2-Pyrimidinyl)-1-piperazinyl]butyl]-8-azaspiro[4.5]decane-7,9-dione
Percent Composition: C 65.43%, H 8.11%, N 18.17%, O 8.30%
Literature References: Non-benzodiazepine anxiolytic; 5-hydroxytryptamine (5-HT1) receptor agonist. Prepn: Y. H. Wu et al., J. Med. Chem. 15, 477 (1972); Y. H. Wu, J. W. Rayburn, DE 2057845 (1971 to Bristol-Myers); eidem, US 3717634 (1973 to Mead-Johnson). Pharmacology: L. E. Allen et al., Arzneim.-Forsch. 24, 917 (1974). Comparison with diazepam in treatment of anxiety: H. L. Goldberg, R. J. Finnerty, Am. J. Psychiatry 136, 1184 (1979); A. F. Jacobson et al., Pharmacotherapy 5, 290 (1985). Nonsynergistic effect with alcohol: T. Seppala et al., Clin. Pharmacol. Ther. 32, 201 (1982). Disposition and metabolism: S. Caccia et al., Xenobiotica 13, 147 (1983). Series of articles on chemistry, pharmacology, addictive potential, and clinical trials: J. Clin. Psychiatry 43, pp 1-116 (1982); on pharmacology, safety and clinical comparison with clorazepate: Am. J. Med. 80, Suppl. 3B, 1-51 (1986). Review of pharmacology and therapeutic efficacy: K. L. Goa, A. Ward, Drugs 32, 114-129 (1986). Review: M. W. Jann, Pharmacotherapy 8, 100-116 (1988); D. P. Taylor, FASEB J. 2, 2445-2452 (1988).