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

Antrafenine CAS Registry Number: 55300-29-3 安曲非宁

CAS Name: 2-[[7-(Trifluoromethyl)-4-quinolinyl]amino]benzoic acid 2-[4-[3-(trifluoromethyl)phenyl]-1-piperazinyl]ethyl ester
Additional Names: 2-[4-(a,a,a-trifluoro-m-tolyl)-1-piperazinyl]ethyl...
Literature References: Analgesic with minimal anti-inflammatory and antipyretic activity, related structurally to floctafenine. Prepn: P. R. L. Giudicelli et al., DE 2415982; eidem, US 3935229 (1974, 1976 both to Synthelabo); P. M. Manoury et al., J. Med. Chem. 22, 554 (1979). Pharmacokinetic study: L. G. Dring et al., Br. J. Pharmacol. 63, 368P (1978). Metabolism: V. Rovei et al., Ann. Chim. 67, 733 (1977). Pharmacologic study: R. D. Sofia et al., Pharmacol. Res. Commun. 11, 179 (1979).

Ciramadol CAS Registry Number: 63269-31-8 西拉马朵

CAS Name: 3-[(R)-(Dimethylamino)[(1R,2R)-2-hydroxycyclohexyl]methyl]phenol
Additional Names: (-)-cis-2-(a-dimethylamino-m-hydroxybenzyl)cyclohexanolPercent Composition: C 72.25%, H 9.30%, N 5.6...
Literature References: Analgesic with narcotic agonist-antagonist properties. Prepn: J. P. Yardley, P. B. Russel, DE 2317183; eidem, US 3928626, US 4017637 (1973, 1975 and 1977 all to Am. Home). Synthesis, relative stereochemistry, biological activity: J. P. Yardley et al., Experientia 34, 1124 (1978). Abs config: W. Stallings, Jr., J. Donohue, J. Cryst. Mol. Struct. 11, 59 (1981). Determn in pharmaceutical dosage forms: H. K. Chan, A. G. Fogg, Anal. Chim. Acta 105, 423 (1979). Metabolism: C. O. Tio et al., Fed. Proc. 38, 2717 (1979). Respiratory effects in man: H. P. Wuest, Arch. Int. Pharmacodyn. Ther. 240, 45 (1979). Analgesic effect in chronic pain: M. J. Staquet, Curr. Med. Res. Opin. 6, 475 (1980).

Pirbuterol CAS Registry Number: 38677-81-5 6-2-(tert-丁胺)-1-羟基-2-(羟甲基)吡啶-3-醇

CAS Name: a6-[[(1,1-Dimethylethyl)amino]methyl]-3-hydroxy-2,6-pyridinedimethanol
Additional Names: 2-hydroxymethyl-3-hydroxy-6-(1-hydroxy-2-tert-butylaminoethyl)pyridine
Percent Composition:...
Literature References: Analog of albuterol, q.v., with b2-adrenergic stimulating activity. Prepn: W. E. Barth, DE 2204195; idem, US 3700681 (both 1972 to Pfizer). Stability study: P. C. Bansal, D. C. Monkhouse, J. Pharm. Sci. 66, 819 (1977). Biotransformation: H. M. McIlhenny, M. S. D. Ghaly, Fed. Proc. 38, 1130 (1979). Pharmacokinetics and cardiopulmonary effects in dogs: J. W. Constantine et al., J. Pharmacol. Exp. Ther. 208, 371 (1979). Comparative study in respiratory disease: A. J. Dyson, A. D. Mackay, Br. J. Dis. Chest 74, 70 (1980). Use in treatment of cardiac failure: N. A. Awan et al., Clin. Res. 28, 17A (1980); W. S. Colucci et al., N. Engl. J. Med. 305, 185 (1981); G. I. Nelson et al., Eur. Heart J. 3, 238 (1982); K. T. Weber et al., Circulation 66, 1262 (1982). Review of pharmacology and efficacy in bronchospastic disease: D. M. Richards, R. N. Brogden, Drugs 30, 6-21 (1985).

Buparvaquone CAS Registry Number: 88426-33-9 布帕伐醌

CAS Name: 2-[[4-(1,1-Dimethylethyl)cyclohexyl]methyl]-3-hydroxy-1,4-naphthalenedione
Additional Names: 2-[(4-tert-butylcyclohexyl)methyl]-3-hydroxy-1,4-naphthoquinone; 3-(4-t-butylcyclohexyl)me...
Literature References: Analog of antimalarial hydroxynaphthoquinones; t-butyl deriv of parvaquone, q.v. Prepn: A. T. Hudson, A. W. Randall, EP 77550; eidem, US 4485117 (1983, 1984 both to Wellcome). In vivo and in vitro antiprotozoal activity: A. T. Hudson et al., Parasitology 90, 45 (1985); N. McHardy et al., Res. Vet. Sci. 39, 29 (1985). Treatment of bovine theileriosis: S. Dhar et al., Vet. Rec. 119, 635 (1986). Efficacy as a chemoimmunoprophylactic of theileriosis: eidem, ibid. 120, 375 (1987).

Triflusal CAS Registry Number: 322-79-2 三氟醋柳酸

CAS Name: 2-(Acetyloxy)-4-(trifluoromethyl)benzoic acid
Additional Names: a,a,a-trifluoro-2,4-cresotic acid acetate; acetyl-4-trifluoromethylsalicylic acidTrademarks: Disgren (Uriach)
Percen...
Literature References: Analog of aspirin, q.v.; inhibits platelet aggregation. Prepn of free acid: M. Hauptschein, US 3019253 (1962 to Pennsalt). Inhibition of platelet aggregation in man and rat: J. Garcia-Rafanell, J. Morell, Therapie 32, 337 (1977). Effect on blood coagulation: M. Rutllant et al., Curr. Ther. Res. 22, 510 (1977). Pharmacokinetics: V. Rimbau et al., Arch. Farmacol. Toxicol. 7, 11 (1981). Clinical studies: R. M. Masso et al., Curr. Ther. Res. 25, 791 (1979); E. Sala-Planell et al., Angiologia 33, 71 (1981).

Plafibride CAS Registry Number: 63394-05-8 普拉贝脲

CAS Name: 2-(4-Chlorophenoxy)-2-methyl-N-[[(4-morpholinylmethyl)amino]carbonyl]propanamide
Additional Names: N-2-(p-chlorophenoxy)isobutyryl-N'-morpholinomethylureaTrademarks: Idonor (Roger); P...
Literature References: Analog of clofibrate, q.v. Prepn: J. Iniesta-Pons, DE 2716374 (1977 to Investigacion Tecnica y Aplicada), C.A. 88, 37810g (1978). Toxicity data: J. Zapatero, L. Brugeghini, Arch. Farmacol. Toxicol. 4, 137 (1978). Series of articles on antiplatelet aggregation activity, hypolipemic activity, pharmacology, and toxicology: ibid., 132-142.

Clobuzarit CAS Registry Number: 22494-47-9 氯丁扎利

CAS Name: 2-[[4'-Chloro(1,1'-biphenyl)-4-yl]methoxy]-2-methylpropanoic acid
Additional Names: 2-[[p-(p-chlorophenyl)benzyl]oxy]-2-methylpropionic acidTrademarks: Clozic (ICI)
Percent Composi...
Literature References: Analog of clofibrate. Prepn: T. Leigh, L. A. McArdle, GB 1140748; eidem, US 3549690 (1969, 1970 both to ICI). Pharmacological studies: M. E. J. Billingham, Br. J. Pharmacol. 72, 523 (1981); M. E. J. Billingham et al., ibid. 551. Effects on platelet function in atherosclerosis: J. R. O'Brien et al., Thromb. Haemostasis 40, 75 (1978). Comparative clinical evaluation with penicillamine: D. Y. Bulgen et al., Ann. Rheum. Dis. 38, 567 (1979); H. A. Bird et al., Clin. Exp. Rheumatol. 1, 93 (1983).

Quinupramine CAS Registry Number: 31721-17-2 奎纽帕明

CAS Name: 5-(1-Azabicyclo[2.2.2]oct-3-yl)-10,11-dihydro-5H-dibenz[b,f]azepine
Additional Names: 10,11-dihydro-5-(3-quinuclidinyl)-5H-dibenz[b,f]azepineTrademarks: Kinupril (Bellon); Kevopril (R...
Literature References: Analog of imipramine, q.v. Prepn: C. Gueremy, P. C. Wirth, DE 2030492 (1971 to Sogeras), C.A. 74, 141581e (1971). Animal studies: W. Van Dorsser, A. Dresse, Arch. Int. Pharmacodyn. Ther. 208, 373 (1974); eidem, ibid. 220, 164 (1976). Clinical study: R. Volmat et al., Clin. Neurol. Psychiat. 239, 445 (1978).

Terlipressin CAS Registry Number: 14636-12-5 特利加压素

CAS Name: N-[N-(N-Glycylglycyl)glycyl]-8-L-lysinevasopressin
Additional Names: Na-glycylglycylglycylvasopressin; 1-triglycyl-8-lysinevasopressin
Trademarks: Glypressin (Ferring)
Percent C...
Literature References: Analog of lypressin, q.v. Prepn: E. Kasafirek et al., Collect. Czech. Chem. Commun. 31, 4581 (1966); Z. Procházka et al., ibid. 43, 1285 (1978). Pharmacological studies: J. Kyncl et al., Eur. J. Pharmacol. 28, 294 (1974); P. O. B. Sjöquist et al., Acta Pharmacol. Toxicol. 40, 369 (1977). Use in treatment of uterine bleeding: V. Pavlin et al., Br. J. Obstet. Gynaecol. 85, 801 (1978). Hemostatic effects in cirrhosis patients: C. V. Prowse et al., Eur. J. Clin. Invest. 10, 49 (1980). Conversion to lysine vasopressin in man: M. L. Forsling et al., J. Endocrinol. 85, 237 (1980). Uterine effects in first trimester of pregnancy: T. Laudanski, M. Aakerlund, Contraception 22, 199 (1980). Single-dose effects on renal potassium excretion in humans: H. Nadvornikova, O. Schueck, Int. J. Clin. Pharmacol. Ther. Toxicol. 20, 155 (1982).

Secnidazole CAS Registry Number: 3366-95-8 塞克硝唑

CAS Name: a,2-Dimethyl-5-nitro-1H-imidazole-1-ethanol
Additional Names: 1-(2-hydroxypropyl)-2-methyl-5-nitroimidazole; 1-(2-methyl-5-nitroimidazol-1-yl)-2-propanolTrademarks: Flagentyl (Rhe-Pou...
Literature References: Analog of metronidazole, q.v. Prepn: FR M3270 (1965 to Rhône-Poulenc), C.A. 63, 11571d (1965); C. Cosar et al., Arzneim.-Forsch. 16, 23 (1966). Anti-amebic and trichomonacidal activities: F. Benazet, L. Guillaume, Bull. Soc. Pathol. Exot. Ses Fil. 69, 309 (1976), C.A. 90, 145922v (1979). Serum half-life: J. Symonds, J. Antimicrob. Chemother. 5, 484 (1979). Therapeutic use: D. Videau et al., Br. J. Vener. Dis. 54, 77 (1978).