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

Alinidine CAS Registry Number: 33178-86-8 烯丙尼定

CAS Name: N-(2,6-Dichlorophenyl)-4,5-dihydro-N-2-propenyl-1H-imidazol-2-amine
Additional Names: 2-(N-allyl-2,6-dichloroanilino)-2-imidazoline; 2-[N-allyl-N-(2,6-dichlorophenyl)amino]-2-imidazol...
Literature References: Specific bradycardic agent; analog of clonidine, q.v. Prepn: H. Stähle et al., DE 1958201; eidem, US 3708485 (1971, 1973 both to Boehringer, Ing.); eidem, J. Med. Chem. 23, 1217 (1980). Clinical pharmacology: D. W. G. Harron et al., J. Cardiovasc. Pharmacol. 4, 213 (1982). Mode of action study: J. S. Millar, E. M. Vaughan Williams, Lancet 1, 1291 (1981). HPLC determn in human plasma: U.-W. Wiegand et al., J. Chromatogr. 223, 238 (1981). Clinical pharmacokinetics: eidem, J. Cardiovasc. Pharmacol. 4, 59 (1982). Hemodynamic effects in angina or infarction: M. L. Simoons, P. G. Hugenholtz, Eur. Heart J. 5, 227 (1984). Review of pharmacology and potential therapeutic uses: D. W. G. Harron, R. G. Shanks, ibid. 6, 722-729 (1985).

Zatebradine CAS Registry Number: 85175-67-3 扎替雷定

CAS Name: 3-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one
Additional Names: 1-(7,8-dimethoxy-1,3,4,5-tetrahydro-2H-3-benzazepin-2-...
Literature References: Specific bradycardic agent; sinus node inhibitor. Prepn: M. Reiffen et al., EP 65229; eidem, US 4490369 (1982, 1984 both to Thomae); and structure-activity study: M. Reiffen et al., J. Med. Chem. 33, 1496 (1990). Pharmacology: W. Kobinger, C. Lillie, Eur. J. Pharmacol. 104, 9 (1984). Mechanism of action study: M. Goethals et al., Circulation 88, 2389 (1993). Pharmacokinetics: W. Roth et al., J. Pharm. Sci. 82, 99 (1993). GC-MS determn in plasma: J. Schmid et al., J. Chromatogr. 658, 93 (1994).

Labetalol CAS Registry Number: 36894-69-6 拉贝洛尔

CAS Name: 2-Hydroxy-5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]benzamide
Additional Names: 5-[1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl]salicylamide; ibidomide
Percent Comp...
Literature References: Specific competitive antagonist at both a- and b-adrenergic receptor sites. Prepn: L. H. Lunts, D. T. Collin, DE 2032642; eidem, US 4012444 (1971, 1977 both to Allen Hanburys). Synthesis of labetalol and enantiomers: J. E. Clifton et al., J. Med. Chem. 25, 670 (1982); and comparison of cardiovascular properties: E. H. Gold et al., ibid. 1363. Abs config of dilevalol: P. Murray-Rust et al., Acta Crystallogr. C40, 825 (1984). Adrenoceptor blocking properties: E. J. Sybertz et al., J. Pharmacol. Exp. Ther. 218, 435 (1981). HPLC determn in serum or plasma: T. F. Woodman, B. Johnson, Ther. Drug Monit. 3, 371 (1981). Metabolism in animals and man: R. Hopkins et al., Biochem. Soc. Trans. 4, 726 (1976). Toxicity: K. Shimpo et al., Hokkaido Igaku Zasshi 53, 15 (l978), C.A. 90, 66465v (1974). Review of pharmacology: R. Donnelly, G. J. A. Macphee, Clin. Pharmacokinet. 21, 95-109 (1991); of therapeutic applications in hypertension and ischemic heart disease: K. L. Goa et al., Drugs 37, 583-627 (1989).

Remoxipride CAS Registry Number: 80125-14-0 瑞莫必利

CAS Name: 3-Bromo-N-[[(2S)-1-ethyl-2-pyrrolidinyl]methyl]-2,6-dimethoxybenzamide
Additional Names: (-)-N-ethyl-2-(3-bromo-2,6-dimethoxybenzamidomethyl)pyrrolidine
Percent Composition: C 51.7...
Literature References: Specific dopamine D2-receptor antagonist. Prepn: G. L. Florvall, S. O. Ogren, EP 4831; eidem, US 4232037 (1979, 1980 both to Astra); eidem, J. Med. Chem. 25, 1280 (1982). Antidopaminergic activity: S. O. Ogren et al., Eur. J. Pharmacol. 102, 459 (1984). Radiometric determn in urine: A. C. Veltkamp et al., J. Chromatogr. 384, 357 (1987). Clinical pharmacology and pharmacokinetics: L. Farde et al., Psychopharmacology 95, 157 (1988). Clinical evaluation in tardive dyskinesia: U. Andersson et al., ibid. 94, 167 (1988); in schizophrenia: R. G. McCreadie et al., Acta Psychiatr. Scand. 78, 49 (1988).

Lamifiban CAS Registry Number: 144412-49-7 醋酸,2-[[1-[(2S)-2-[[4-(氨基亚胺甲基)苯甲酰]氨基]-3-(4-羟基苯基)-1-氧丙基]-4-哌啶基]-

CAS Name: (S)-[[1-[2-[[4-(Aminoiminomethyl)benzoyl]amino]-3-(4-hydroxyphenyl)-1-oxopropyl]-4-piperidinyl]oxy]acetic acid
Additional Names: [[1-[N-(p-amidinobenzoyl)-L-tyrosyl]-4-piperidinyl]oxy...
Literature References: Specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Prepn: L. Alig et al., EP 505868; eidem, US 5378712 (1992, 1995 both to Hoffmann-La Roche); L. Alig et al., J. Med. Chem. 35, 4393 (1992). Pharmacology: J.-P. Carteaux et al., Thromb. Haemostasis 70, 817 (1993); Y. Takiguchi et al., ibid. 73, 683 (1995).

Tirofiban CAS Registry Number: 144494-65-5 替罗非班

CAS Name: N-(Butylsulfonyl)-O-[4-(4-piperidinyl)butyl]-L-tyrosine
Additional Names: N-(butylsulfonyl)-4-[4-(4-piperidyl)butoxy]-L-phenylalanine; 2-S-(n-butylsulfonylamino)-3-[4-(piperidin-4-yl)...
Literature References: Specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Prepn: M. S. Egbertson et al., EP 478363; M. E. Duggan et al., US 5292756 (1992, 1994 both to Merck Co.); J. Y. L. Chung et al., Tetrahedron 49, 5767 (1993). Physicochemical properties: J. A. McCauley et al., J. Phys. D: Appl. Phys. 26, B85 (1993). Pharmacology: J. J. Lynch et al., J. Pharmacol. Exp. Ther. 272, 20 (1995). Clinical pharmacokinetics and pharmacodynamics: J. S. Barrett et al., Clin. Pharmacol. Ther. 56, 377 (1994). Clinical trials in angina: P. Théroux et al., N. Engl. J. Med. 338, 1488 (1998); H. D. White et al., ibid. 1498. Clinical comparison with abciximab, q.v., in coronary revascularization: D. J. Moliterno et al., Lancet 360, 355 (2002).

Lotrafiban CAS Registry Number: 171049-14-2 洛曲非班

CAS Name: (2S)-7-([4,4'-Bipiperidin]-1-ylcarbonyl)-2,3,4,5-tetrahydro-4-methyl-3-oxo-1H-1,4-benzodiazepine-2-acetic acidPercent Composition: C 64.47%, H 7.53%, N 13.07%, O 14.93%
Literature References: Specific nonpeptide platelet fibrinogen receptor (GPIIb/IIIa) antagonist. Prepn: W. E. Bondinell et al., WO 9518619; W. E. Bondinell, J. M. Samanen, US 6117866 (1995, 2000 both to SmithKline Beecham). Enantiospecific synthesis: W. H. Miller et al., Tetrahedron Lett. 36, 9433 (1995). Structure-activity study: J. M. Samanen et al., J. Med. Chem. 39, 4867 (1996). Binding study: A. Wong et al., J. Pharmacol. Exp. Ther. 285, 228 (1998). Clinical evaluation in patients with coronary or cerebral atherosclerosis: R. A. Harrington et al., Circulation 102 728 (2000). Clinical trial in cerebrovascular and coronary artery disease: E. J. Topol et al., Circulation 108, 399 (2003).

Cangrelor CAS Registry Number: 163706-06-7 坎格雷洛

CAS Name: N-[2-(Methylthio)ethyl]-2-[(3,3,3-trifluoropropyl)thio]-5'-adenylic acid monoanhydride with (dichloromethylene)bis[phosphonic acid]
Additional Names: N6-(2-methylthioethyl)-2-(3,3,3-t...
Literature References: Specific P2Y12 purinoceptor antagonist; inhibits ADP-induced platelet aggregation. Prepn: A. H. Ingall et al., WO 9418216 (1994 to Fisons); eidem, US 5721219 (1998 to Astra); and in vivo antithrombotic activity: idem et al., J. Med. Chem. 42, 213 (1999). In vivo antithrombotic effects in canine arterial thrombosis: J. Huang et al., J. Pharmacol. Exp. Ther. 295, 492 (2000). Mechanism of action study: A. Ishii-Watabe et al., Biochem. Pharmacol. 59, 1345 (2000). Clinical safety assessment and evaluation in acute coronary syndromes: R. F. Storey et al., Thromb. Haemostasis 85, 401 (2001); in angina pectoris and non-Q-wave myocardial infarction: F. Jacobsson et al., Clin. Ther. 24, 752 (2002). Clinical pharmacodynamics compared with clopidogrel: R. F. Storey et al., Platelets 13, 407 (2002). Review of clinical development: S. C. Chattaraj, Curr. Opin. Invest. Drugs 2, 250-255 (2001).

Ketanserin CAS Registry Number: 74050-98-9 凯他色林

CAS Name: 3-[2-[4-(4-Fluorobenzoyl)-1-piperidinyl]ethyl]-2,4[1H,3H]-quinazolinedioneTrademarks: Ketensin (Janssen); Serefrex (Janssen); Taseron (Janssen)
Percent Composition: C 66.82%, H 5.61%,...
Literature References: Specific serotonin (5HT2)-receptor antagonist. Prepn: J. Vandenbeck et al., EP 13612; eidem, US 4335127 (1980, 1982 both to Janssen). X-ray structure: O. M. Peeters et al., Cryst. Struct. Commun. 11, 375 (1982). Receptor binding profile: J. E. Leysen et al., Life Sci. 28, 1015 (1981). Pharmacology: J. M. Van Neuten et al., J. Pharmacol. Exp. Ther. 218, 217 (1981). HPLC determn in plasma: A. T. Kacprowicz et al., J. Chromatogr. 272, 417 (1983). Clinical efficacy in intermittent claudication: J. De Cree et al., Lancet 2, 775 (1984); in Raynaud's phenomenon: J. R. Seibold, A. H. M. Jageneau, Arthritis Rheum. 27, 139 (1984); in hypertension: A. Amery et al., J. Cardiovasc. Pharmacol. 6, 182 (1984). Series of articles on pharmacology and clinical studies: ibid. 7, Suppl. 7, S1-S182 (1985); on pharmacokinetics and metabolism: Arzneim.-Forsch. 38, 775-800 (1988). Review of pharmacology and clinical efficacy in hypertension and vascular disease: R. N. Brogden, E. M. Sorkin, Drugs 40, 903-949 (1990).

Granisetron CAS Registry Number: 109889-09-0 格拉司琼

CAS Name: 1-Methyl-N-[(3-endo)-9-methyl-9-azabicyclo[3.3.1]non-3-yl]-1H-indazole-3-carboxamide
Percent Composition: C 69.20%, H 7.74%, N 17.93%, O 5.12%
Literature References: Specific serotonin (5HT3) receptor antagonist. Prepn: F. D. King, EP 200444; idem, US 4886808 (1986, 1989 both to Beecham). 5HT3 receptor binding study: G. J. Kilpatrick et al., Nature 330, 746 (1987). Series of articles on pharmacology and clinical trials to prevent chemotherapy-induced emesis: Semin. Oncol. 22, Suppl. 10, 1-30 (1995).