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

Citalopram CAS Registry Number: 59729-33-8 西酞普兰

CAS Name: 1-[3-(Dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-isobenzofurancarbonitrile
Additional Names: 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-5-phthalancarbonitrile; nitalap...
Literature References: Selective serotonin reuptake inhibitor (SSRI). Prepn: K. P. Boegesoe, A. S. Toft, DE 2657013; eidem, US 4136193 (1977, 1979 both to Kefalas); A. J. Bigler et al., Eur. J. Med. Chem. - Chim. Ther. 12, 289 (1977). Prepn of enantiomers: K. P. Boegesoe, J. Perregaard, EP 347066; eidem, US 4943590, reissued as US RE 34712 (1989, 1990, 1994 all to Lundbeck). Pharmacology: A. V. Christensen et al., Eur. J. Pharmacol. 41, 153 (1977). HPLC determn in plasma and urine: E. Oyehaug et al., J. Chromatogr. 308, 199 (1984). Comparative biotransformation of enantiomers: L. L. Von Moltke et al., Drug Metab. Dispos. 29, 1102 (2001). Review of clinical pharmacokinetics: K. Brosen, C. A. Naranjo, Eur. Neuropsychopharmacol. 11, 275-283 (2001). Review of clinical experience in depression: M. B. Keller, J. Clin. Psychiatry 61, 896-908 (2000). Clinical trial of S-form in depression: W. J. Burke et al, ibid. 63, 331 (2002).

Chlorimuron-ethyl CAS Registry Number: 90982-32-4 氯嘧磺隆

CAS Name: 2-[[[[(4-Chloro-6-methoxy-2-pyrimidinyl)amino]carbonyl]amino]sulfonyl]benzoic acid ethyl ester
Additional Names: ethyl 2-[[[[(4-chloro-6-methoxypyrimidin-2-yl)amino]carbonyl]amino]sul...
Literature References: Selective sulfonylurea herbicide. Prepn: A. D. Wolf, AT 8316181; idem, US 4547215 (1984, 1985 both to Du Pont). Effect on plant growth and pigment synthesis: R. M. Devlin, Z. K. Koszanski, Proc. Annu. Meet. Northeast. Weed Sci. Soc. 40, 115 (1986). Metabolism by plants: H. M. Brown, S. M. Neighbors, Pestic. Biochem. Physiol. 29, 112 (1987). Field trial in soybeans: G. N. Rhodes et al., Tenn. Farm Home Sci. 142, 21 (1987). HPLC determn in crops: J. L. Prince, R. A. Guinivan, J. Agric. Food Chem. 36, 63 (1988). Brief review: J. S. Claus, Weed Technol. 1, 114-115 (1987).

Flonicamid CAS Registry Number: 158062-67-0 氟啶虫酰胺

CAS Name: N-(Cyanomethyl)-4-(trifluoromethyl)-3-pyridinecarboxamide
Additional Names: N-(cyanomethyl)-4-(trifluoromethyl)nicotinamideTrademarks: Aria (FMC); Urara (ISK)
Percent Composition: ...
Literature References: Selective systemic aphicide. Prepn: T. Toki et al., EP 580374; eidem, US 5360806 (both 1994 to Ishihara Sangyo Kaisha). Comprehensive description: M. Morita et al., BCPC Conf. - Pests Dis. 2000, 59-65. Field performance in cotton: H. G. Hancock, Proc. Beltwide Cotton Conf. 2004, 1629.

Dalapon CAS Registry Number: 75-99-0 2,2-二氯丙酸

CAS Name: 2,2-Dichloropropanoic acid
Additional Names: a,a-dichloropropionic acid
Percent Composition: C 25.20%, H 2.82%, Cl 49.60%, O 22.38%
Literature References: Selective systemic herbicide for control of annual and perennial grasses. Prepn: GB 752761 (1956 to Dow); E. J. Kowolik, J. W. Fisher, GB 892584 (1962 to British Celanese); of free acid and sodium salt: Smeykal, Pallutz, Chem. Tech. (Leipzig) 15 (11), 654 (1963), C.A. 60, 6741c (1964). Acute toxicity: T. B. Gaines, R. E. Linder, Fundam. Appl. Toxicol. 7, 299 (1986). Toxicity data for the sodium salt: G. W. Bailey, J. L. White, Residue Rev. 10, 97 (1965). Quantitative NMR purity determn: R. J. Wells et al., J. Agric. Food Chem. 50, 3366 (2002).

Mibefradil CAS Registry Number: 116644-53-2 米贝地尔

CAS Name: Methoxyacetic acid (1S,2S)-2-[2-[[3-(1H-benzimidazol-2-yl)propyl]methylamino]ethyl]-6-fluoro-1,2,3,4-tetrahydro-1-(1-methylethyl)-2-naphthalenyl ester
Additional Names: (1S,2S)-2-[2-[...
Literature References: Selective T-type calcium channel blocker. Prepn: Q. Branca et al., EP 268148; eidem, US 4808605 (1988, 1989 both to Hoffmann-La Roche). Calcium channel selectivity: S. K. Mishra, K. Hermsmeyer, Circ. Res. 75, 144 (1994). Metabolism in rats: H. R. Wiltshire et al., Xenobiotica 22, 837 (1992). Review of pharmacology, toxicology and clinical evaluation: J.-P. Clozel et al., Cardiovasc. Drug Rev. 9, 4-17 (1991); of pharmacology and pharmacokinetics: D. R. Abernethy, Am. J. Cardiol. 80, 4C-11C (1997); of clinical trials in hypertension: S. Oparil, Am. J. Hypertens. 11, 88S-94S (1998); in chronic stable angina pectoris: B. M. Massie, ibid. 95S-102S. Post-marketing safety assessment: J. Riley et al., Int. J. Clin. Pharmacol. Ther. 40, 241 (2002).

Tadalafil CAS Registry Number: 171596-29-5 他达那非

CAS Name: (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methylpyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione
Additional Names: (6R,12aR)-2,3,6,7,12,12a-hexahydro-2-methyl-6-[3...
Literature References: Selective type 5 cGMP phosphodiesterase (PDE-5) inhibitor. Prepn: A. C. Daugan, WO 9519978 (1995 to Glaxo); eidem, US 5859006 (1999 to ICOS); and PDE-5 inhibition: idem et al., J. Med. Chem. 46, 4525, 4533 (2003). HPLC determn in plasma: C.-L. Cheng, C.-H. Chou, J. Chromatogr. B 822, 278 (2005). Clinical pharmacokinetics: S. T. Forgue et al., Br. J. Clin. Pharmacol. 61, 280 (2005). Clinical trial in erectile dysfunction: G. B. Brock et al., J. Urol. 168, 1332 (2002); in comparison with sildenafil: I. Eardley et al., BJU Int. 96, 1323 (2005). Review of pharmacology and clinical experience: H. Porst, Int. J. Impotence Res. 14, Suppl. 1, S57-S64 (2002); in comparison with other phosphodiesterase inhibitors: S. A. Doggrell, Expert Opin. Pharmacother. 6, 75-84 (2005).

Fluthiacet-methyl CAS Registry Number: 117337-19-6 嗪草酸甲酯

CAS Name: [[2-Chloro-4-fluoro-5-[(tetrahydro-3-oxo-1H,3H-[1,3,4]thiadiazolo[3,4-a]pyridazin-1-ylidene)amino]phenyl]thio]acetic acid methyl ester
Additional Names: 9-(4-chloro-2-fluoro-5-methoxy...
Literature References: Selective, post-emergence, isourazole herbicide which upon conversion to the urazole inhibits protoporphyrinogen oxidase. Prepn: M. Yamaguchi et al., EP 273417; eidem, US 4906279 (1988, 1990 both to Kumiai Chem. Ind.; Ihara Chem. Ind.). Description of physical properties, toxicity, and activity: T. Miyazawa et al., Brighton Crop Prot. Conf. - Weeds 1993, 23. Conversion to active metabolite and mode of action study: T. Shimizu et al., Plant Cell Physiol. 36, 625 (1995). Field study as harvest-aid for cotton: R. G. Lemon et al., Proc. Beltwide Cotton Conf. 1999, 605.

Isoxaben CAS Registry Number: 82558-50-7 异噁酰草胺

CAS Name: N-[3-(1-Ethyl-1-methylpropyl)-5-isoxazolyl]-2,6-dimethoxybenzamide
Additional Names: benzamizoleTrademarks: Flexidor (Dow AgroSci.); Gallery (Dow AgroSci.)
Percent Composition: C 6...
Literature References: Selective, pre-emergent herbicide for broadleaf weeds and annual grasses. Prepn: K. W. Burow, GB 2084140; see also: idem, US 4636243 (1982, 1987 both to Lilly). Physical properties and herbicidal activity: F. Huggenberger et al., Proc. Br. Crop Prot. Conf. - Weeds 1982, 47. Mobility and degradation in soil: F. Huggenberger, P. J. Ryan, ibid. 1985, 947. Effect on cellular growth and metabolism: A. Lefebvre et al., Weed Res. 27, 125 (1987). Field trials: F. Huggenberger, F. Gueguen, Crop Prot. 6, 75 (1987); F. O. Colbert, D. H. Ford, Proc. West. Soc. Weed Sci. 40, 155 (1987).

Ethalfluralin CAS Registry Number: 55283-68-6 丁氟消草

CAS Name: N-Ethyl-N-(2-methyl-2-propenyl)-2,6-dinitro-4-(trifluoromethyl)benzenamine
Additional Names: N-ethyl-N-a,a,a-trifluoro-N-(2-methylallyl)-2,6-dinitro-p-toluidine; N-ethyl-N-methallyl-4...
Literature References: Selective, pre-emergent herbicide. Prepn: H. D. Porter, DE 2511897; idem, GB 1505249 (1975, 1978 both to Eli Lilly). Activity: G. Skylakakis et al., Proc. 12th Br. Weed Control Conf. 2, 795 (1974). Review of chemistry and analytical methods: E. W. Day, "Ethalfluralin" in Analytical Methods for Pesticides and Plant Growth Regulators Vol. 10, G. Zweig, J. Sherma, Eds. (Academic Press, New York, 1978) pp 341-352. Persistence in soil: B. J. Hayden, A. E. Smith, Bull. Environ. Contam. Toxicol. 25, 508 (1983).

Carmoxirole CAS Registry Number: 98323-83-2 3-[4-(3,6-二氢-4-苯基-1(2H)-吡啶)丁基]-1H-吲哚-5-羧酸盐酸盐

CAS Name: 3-[4-(3,6-Dihydro-4-phenyl-1(2H)-pyridinyl)butyl]-1H-indole-5-carboxylic acid
Percent Composition: C 76.98%, H 7.00%, N 7.48%, O 8.54%
Literature References: Selective, presynaptic dopamine D2-receptor agonist. Prepn: H. Böttcher et al., DE 3342632; eidem, US 5256673 (1985, 1993 both to E. Merck); H. Böttcher, R. Gericke, Ann. 1988, 749. Neurochemical profile: A. F. Haase et al., Arch. Pharmacol. 343, 588 (1991). Pharmacology: G. Haeusler et al., Eur. Heart J. 13, Suppl. D, 129 (1992). Pharmacokinetics and clinical evaluation: W. Meyer et al., ibid. 121.