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

Iomeprol CAS Registry Number: 78649-41-9 碘美普尔

CAS Name: N,N'-Bis(2,3-dihydroxypropyl)-5-[(hydroxyacetyl)methylamino]-2,4,6-triiodo-1,3-benzenedicarboxamide
Additional Names: N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-5-(N-methylglycolamid...
Literature References: Nonionic x-ray contrast media. Prepn: E. Felder, D. Pitrè, EP 026281; eidem, US 4352788 (1981, 1982 both to Bracco). HPLC determn in plasma and urine: V. Lorusso et al., J. Chromatogr. 525, 401 (1990). Series of articles on properties, pharmacology, pharmacokinetics and clinical experience in angiography and urography: Eur. J. Radiol. 18, Suppl. 1, S1-S124 (1994). Toxicology study: A. Morisetti et al., ibid. S21.

Iodixanol CAS Registry Number: 92339-11-2 碘克沙醇

CAS Name: 5,5'-[(2-Hydroxy-1,3-propanediyl)bis(acetylimino)]bis[N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-1,3-benzenedicarboxamide]
Additional Names: 5,5'-[(2-hydroxytrimethylene)bis(acetylim...
Literature References: Nonionic, dimeric x-ray contrast medium. Prepn: P. E. Hansen et al., EP 108638 (1984 to Nyegaard), C.A. 101, 151599g (1984). HPLC determn in plasma: H. Nomura et al., J. Chromatogr. 572, 333 (1991). Clinical pharmacokinetics: M. G. Svaland et al., Invest. Radiol. 27, 130 (1992). Clinical studies in cerebral arteriography: Y. Palmers et al., Eur. J. Radiol. 17, 203 (1993); in cardiac angiography: J. A. Hill et al., Am. J. Cardiol. 74, 57 (1994); in urography: R. M. Conroy et al., Clin. Radiol. 49, 337 (1994). Use as density gradient medium: T. Ford et al., Anal. Biochem. 220, 360 (1994); J. Graham et al., ibid. 367.

Iopromide CAS Registry Number: 73334-07-3 碘普罗胺

CAS Name: N,N'-Bis(2,3-dihydroxypropyl)-2,4,6-triiodo-5-[(methoxyacetyl)amino]-N-methyl-1,3-benzenedicarboxamide
Additional Names: N,N'-bis(2,3-dihydroxypropyl)-2,4,6-triiodo-5-(2-methoxyacetam...
Literature References: Nonionic, injectable radio-contrast medium. Prepn: U. Speck et al., DE 2909439; eidem, US 4364921 (1980, 1982 both to Schering AG). Physicochemical properties and pharmacological profile: W. Muetzel, U. Speck, Am. J. Neuroradiol. 4, 350 (1983); P. Dawson et al., Acta Radiol. Diagn. 25, 253 (1984). Clinical experience: K.-J. Wolf et al., ibid. 24, 55 (1983).

Efavirenz CAS Registry Number: 154598-52-4 依法韦仑

CAS Name: (4S)-6-Chloro-4-(cyclopropylethynyl)-1,4-dihydro-4-(trifluoromethyl)-2H-3,1-benzoxazin-2-oneTrademarks: Stocrin (Merck Co.); Sustiva (BMS)
Percent Composition: C 53.27%, H 2.87%, Cl ...
Literature References: Nonnucleoside HIV-1 reverse transcriptase inhibitor. Prepn: S. D. Young et al., EP 582455; eidem, US 5519021 (1994, 1996 both to Merck Co.). Pharmacology: S. D. Young et al., Antimicrob. Agents Chemother. 39, 2602 (1995). Enantioselective synthesis: A. S. Thompson et al., Tetrahedron Lett. 36, 8937 (1995). Total synthesis and resolution of enantiomers: L. A. Radesca et al., Synth. Commun. 27, 4373 (1997). Ionization behavior: S. R. Rabel et al., Pharm. Dev. Technol. 1, 91 (1996). Clinical trial as component of combination therapy in HIV-1 infection in adults: S. Staszewski et al., N. Engl. J. Med. 341, 1865 (1999); in children: S. E. Starr et al., ibid. 1874. Review of clinical experience: C. Fortin, V. Joly, Expert Rev. Anti Infect. Ther. 2, 671-684 (2004).

Nevirapine CAS Registry Number: 129618-40-2 奈韦拉平

CAS Name: 11-Cyclopropyl-5,11-dihydro-4-methyl-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-oneTrademarks: Viramune (Roxane)
Percent Composition: C 67.65%, H 5.30%, N 21.04%, O 6.01%
Literature References: Non-nucleoside reverse transcriptase inhibitor (NNRTI) of the dipyridodiazepinone class. Prepn: K. D. Hargrave et al., EP 429987 (1991 to Boehringer, Ing; Thomae); eidem, US 5366972 (1994 to Boehringer, Ing.); eidem, J. Med. Chem. 34, 2231 (1991). Inhibition of HIV-1 reverse transcriptase: V. J. Merluzzi et al., Science 250, 1411 (1990). Studies of structure-activity and binding site: P. M. Grob et al., AIDS Res. Hum. Retroviruses 8, 145 (1992). HPLC determn in serum: R. M. Lopez et al., J. Chromatogr. B 751, 371 (2001). Clinical pharmacokinetics: S. H. Cheeseman et al., Antimicrob. Agents Chemother. 37, 178 (1993). Review of clinical experience: A. Carr, D. A. Cooper, Adv. Exp. Med. Biol. 394, 299-304 (1996); of safety profile: R. B. Pollard et al., Clin. Ther. 20, 1071-1092 (1998). Clinical trial in prevention of perinatal HIV-1 transmission: L. A. Guay et al., Lancet 354, 795 (1999).

Tebanicline CAS Registry Number: 198283-73-7 替巴克兰

CAS Name: 5-[(2R)-2-Azetidinylmethoxy]-2-chloropyridinePercent Composition: C 54.42%, H 5.58%, Cl 17.85%, N 14.10%, O 8.05%
Literature References: Non-opioid 3-pyridyl ether analgesic acting acting via a neuronal nicotinic acetylcholine receptor mediated mechanism. Prepn: M. W. Holladay et al., WO 9640682; M. A. Abreo et al., US 5948793 (1996, 1999 both to Abbott); as hydrochloride: M. W. Holladay et al., J. Med. Chem. 41, 407 (1998). Asymmetric synthesis: J. K. Lynch et al., Tetrahedron: Asymmetry 9, 2791 (1998). Analgesic activity and receptor affinity: A. W. Bannon et al., Science 279, 77 (1998). Pharmacology in vitro: D. L. Donnelly-Roberts et al., J. Pharmacol. Exp. Ther. 285, 777 (1998); in vivo: A. W. Bannon et al., ibid. 787. Efficacy in neuropathic pain models: idem et al., Brain Res. 801, 158 (1998).

Perfluoropropane CAS Registry Number: 76-19-7 八氟丙烷

CAS Name: Octafluoropropane
Additional Names: 1,1,1,2,2,3,3,3-octafluoropropane; perflutrenTrademarks: Ispan (Scott Med. Prod.)
Percent Composition: C 19.16%, F 80.84%
Literature References: Non-ozone depleting fluorocarbon; formulated for surgical and diagnostic use. Prepn: J. H. Simons, L. P. Block, J. Am. Chem. Soc. 61, 2962 (1939). See also: J. H. Simons, US 2456027 (1948 to Minnesota Mining Manuf). Physical properties: J. A. Brown, J. Chem. Eng. Data 8, 106 (1963). Thermophysical properties: D. R. Defibaugh, M. R. Moldover, ibid. 42, 160 (1997). Clinical experience in repair of retinal detachment: N. R. Sabates et al., Retina 16, 7 (1996). Review of properties and description: Matheson Gas Data Book, W. Braker, A. L. Mossman, Eds. (Matheson, Lyndhurst, NJ, 6th ed., 1980) p 590-595; of electron interactions for modeling behavior: L. G. Christophorou, J. K. Oltoff, J. Phys. Chem. Ref. Data 27, 889-913 (1998).

Tolvaptan CAS Registry Number: 150683-30-0 托伐普坦

CAS Name: N-[4-[(7-Chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylbenzamide
Additional Names: 7-chloro-5-hydroxy-1-[2-methyl-4-(2-methylbenzoylamino)...
Literature References: Nonpeptide arginine vasopressin V2 receptor antagonist. Prepn: H. Ogawa et al., WO 9105549; eidem, US 5258510 (1991, 1993 both to Otsuka); K. Kondo et al., Bioorg. Med. Chem. 7, 1743 (1999). Pharmacology: Y. Yamamura et al., J. Pharmacol. Exp. Ther. 287, 860 (1998). Clinical trial in heart failure: M. Gheorghiade et al., J. Am. Med. Assoc. 291, 1963 (2004).

Ambrisentan CAS Registry Number: 177036-94-1 安倍生坦

CAS Name: (aS)-a-[(4,6-Dimethyl-2-pyrimidinyl)oxy]-b-methoxy-b-phenylbenzenepropanoic acidPercent Composition: C 69.83%, H 5.86%, N 7.40%, O 16.91%
Literature References: Nonpeptide endothelin ETA receptor antagonist. Prepn: H. Riechers et al., WO 9611914; eidem, US 5932730 (1996, 1998 both to BASF); H. Riechers et al., J. Med. Chem. 39, 2123 (1996). Pharmacology: H. Vatter et al., Clin. Neuropharmacol. 26, 73 (2003). Clinical evaluation in pulmonary arterial hypertension: N. Galié et al., J. Am. Coll. Cardiol. 46, 529 (2005). Review of development and therapeutic potential: G. E. Billman, Curr. Opin. Invest. Drugs 3, 1483-1486 (2002).

Nafamostat CAS Registry Number: 81525-10-2 萘莫司他

CAS Name: 4-[(Aminoiminomethyl)amino]benzoic acid 6-(aminoiminomethyl)-2-naphthalenyl ester
Additional Names: 6-amidino-2-naphthyl-4-guanidinobenzoate; nafamstat
Percent Composition: C 65.69...
Literature References: Non-peptide protease inhibitor. Prepn: S. Fujii et al., EP 48433; eidem, US 4454338 (1982, 1984 both to Torii Co.); T. Aoyama et al., Chem. Pharm. Bull. 33, 1458 (1985). Inhibitory effects on trypsin, thrombin, kallikrein, plasmin and complement-mediated hemolysis: S. Fujii, Y. Hitomi, Biochim. Biophys. Acta 661, 342 (1981); T. Aoyama et al., Jpn. J. Pharmacol. 35, 203 (1984). Effect in experimental acute pancreatitis in rats: M. Iwaki et al., ibid. 41, 155 (1986). Spectrofluorometric determn in biological material: T. Aoyama et al., Chem. Pharm. Bull. 33, 2142 (1985). Clinical anti-complement activity: Y. Miyamoto et al., Trans. Am. Soc. Artif. Intern. Organs 31, 508 (1985).