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

Algestone Acetophenide CAS Registry Number: 24356-94-3 苯甲孕酮

CAS Name: [16a(R)]-16,17-[(1-Phenylethylidene)bis(oxy)]pregn-4-ene-3,20-dione
Additional Names: 16a,17-dihydroxypregn-4-ene-3,20-dione cyclic acetal with acetophenone; 16a,17a-dihydroxyprogeste...
Literature References: Progestogen. Prepn: J. Fried, US 2941997 (1960 to Olin Mathieson); J. Fried et al., Chem. Ind. (London) 1961, 465. Improved prepn: IE 6800457; S. J. Brancato et al., US 3488347 (1968, 1970 both to Smith Kline French). In estrus synchronization: J. N. Wiltbank et al., J. Anim. Sci. 26, 764 (1967). Clinical evaluations of combination with estradiol enanthate as injectable contraceptive: R. Plesner, Acta Endocrinol. 61, 494 (1969); idem, ibid. 65, 683 (1970); R. Recio et al., Contraception 33, 579 (1986).

Arotinolol CAS Registry Number: 68377-92-4 阿罗洛尔

CAS Name: 5-[2-[[3-[(1,1-Dimethylethyl)amino]-2-hydroxypropyl]thio]-4-thiazolyl]-2-thiophenecarboxamide
Additional Names: 2-(3'-tert-butylamino-2'-hydroxypropylthio)-4-(5'-carbamoyl-2'-thienyl)...
Literature References: Propanolamine deriv with a- and b-adrenergic blocking activity. Prepn: T. Hibino et al., DE 2341753; eidem, US 3932400 (1974, 1976 both to Sumitomo); Y. Hara et al., J. Pharm. Sci. 67, 1334 (1978). Characterization of adrenoceptor blocking effects in vivo: A. Miyagishi et al., Arch. Int. Pharmacodyn. Ther. 271, 249 (1984). Possible antianginal effects: M. Sakanashi et al., Oyo Yakuri 28, 709 (1984); C.A. 102, 39669z (1985). Long-term antihypertensive effect in rats: K. Kishi et al., J. Pharmacobio-Dyn. 8, 50 (1985). Comparison with timolol, q.v., of effect on intraocular pressure and hemodynamics: M. Nakashima et al., Eur. J. Clin. Pharmacol. 28, 391 (1985).

Vedaprofen CAS Registry Number: 71109-09-6 维达洛芬

CAS Name: 4-Cyclohexyl-a-methyl-1-naphthaleneacetic acid
Additional Names: 2-(4-cyclohexyl-1-naphthyl)-propionic acidTrademarks: Quadrisol (Intervet)
Percent Composition: C 80.81%, H 7.85%, ...
Literature References: Propionic acid type non-steroidal anti-inflammatory drug (NSAID). Prepn: J. J. Godfroid, E. Steiner, BE 870553; eidem, US 4218473 (1979, 1980 both to CERM). Summary of field trials in dogs: J. G. H. Bergman, P. van Laar, Vet. Q. 18, S20 (1996). Pharmacodynamics and pharmacokinetics in horses: P. Lees et al., J. Vet. Pharmacol. Ther. 22, 96 (1999).

Acetimidoquinone CAS Registry Number: 50700-49-7 N-乙酰苯醌亚胺

CAS Name: N-(4-oxo-2,5-cyclohexadien-1-ylidene)acetamide
Additional Names: N-acetyl-p-benzoquinonimine; N-acetylimidoquinone; NAPQI
Percent Composition: C 64.42%, H 4.73%, N 9.39%, O 21.45%
Literature References: Proposed "ultimate" toxic metabolite of acetaminophen, q.v. Initially prepared by oxidation of acetaminophen with lead tetraacetate and characterized as a Diels-Alder adduct: I. C. Calder et al., J. Med. Chem. 16, 499 (1973). Electrochemical generation in buffer: D. J. Miner, P. T. Kissinger, Biochem. Pharmacol. 28, 3285 (1979). Synthesis in stable benzene soln and reactivity: I. A. Blair et al., Tetrahedron Lett. 21, 4947 (1980). Prepn in cryst form, decomposition kinetics, preliminary toxicological studies: D. C. Dahlin, S. D. Nelson, J. Med. Chem. 25, 885 (1982). Microsomal reactivity study: G. B. Corcoran, Adv. Exp. Med. Biol. 136B, 1085 (1982). Review of acetaminophen-induced hepatotoxicity: J. A. Hinson et al., Life Sci. 29, 107-116 (1981).

Berbine CAS Registry Number: 483-49-8 四氢原小蘖碱

CAS Name: 5,8,13,13a-Tetrahydro-6H-dibenzo[a,g]quinolizine
Additional Names: tetrahydroprotoberberine
Percent Composition: C 86.77%, H 7.28%, N 5.95%
Literature References: Proposed as parent substance for naming berberine and similar alkaloids: Awe, Arch. Pharm. 270, 156 (1932). Synthesis: Chakravarti et al., J. Chem. Soc. 1927, 2278.

Exametazime CAS Registry Number: 105613-48-7 依沙美肟

CAS Name: (2E,2'E,3R,3'R)-rel-3,3'-[(2,2-Dimethyl-1,3-propanediyl)diimino]bis-2-butanone dioxime
Additional Names: (RR,SS)-4,8-diaza-3,6,6,9-tetramethylundecane-2,10-dione bisoxime; (±)-(3...
Literature References: Propyleneamine oxime derivative that forms a neutral, lipophilic complex with 99mTc which diffuses across cellular membranes, including the blood brain barrier. Used in regional cerebral blood flow imaging. Prepn: L. R. Canning et al., EP 194843; eidem, US 4789736 (1986, 1988 both to Amersham). Prepn and ra-diopharmacology of 99mTc complex: D. P. Nowotnik et al., Nucl. Med. Commun. 6, 499 (1985); R. D. Neirinckx et al., J. Nucl. Med. 28, 191 (1987). Clinical comparison of isomers: P. F. Sharp et al., ibid. 27, 171 (1986). Biodistribution in humans: K. Nakamura et al., Eur. J. Nucl. Med. 15, 100 (1989). Clinical evaluation in single photon emission tomography (SPECT) of meningiomas: S. Nakano et al., J. Nucl. Med. 30, 1101 (1989). 99mTc radiolabeling of human platelets: H. J. Danpure, S. Osman, Nucl. Med. Commun. 9, 267 (1988); of human leukocytes: H. J. Danpure et al., ibid. 465. Clinical study of labeled leukocytes for imaging inflammatory lesions: J. H. Reynolds, Clin. Radiol. 42, 195 (1990). Series of articles on basic and clinical studies: J. Cereb. Blood Flow Metab. 8, S1-S126 (1988).

Iloprost CAS Registry Number: 78919-13-8 伊洛前列素

CAS Name: 5-[Hexahydro-5-hydroxy-4-(3-hydroxy-4-methyl-1-octen-6-ynyl)-2(1H)-pentalenylidene]pentanoic acid
Additional Names: 5-(E)-(1S,5S,6R,7R)-7-hydroxy-6-[(E)-(3S,4RS)-3-hydroxy-4-methyl-1-...
Literature References: Prostacyclin analog; 1:1 mixture of 16a- and 16b-methyl diastereomers. Prepn: W. Skuballa et al., DE 2845770; eidem, US 4692464 (1980, 1987 both to Schering AG); W. Skuballa, H. Vorbrüggen, Adv. Prostaglandin Thromboxane Leukotriene Res. 11, 299 (1983). Antithrombotic and cardiovascular pharmacology: K. Schrör et al., Arch. Pharmacol. 316, 252 (1981). Review of clinical pharmacology and pharmacokinetics: S. M. Grant, K. L. Goa, Drugs 43, 889-924 (1992). Clinical study in limb ischemia: J. Dormandy, Therapie 46, 319 (1991); in Raynaud phenomenon: F. M. Wigley et al., Ann. Intern. Med. 120, 199 (1994); in pulmonary hypertension: H. Olschewski et al., N. Engl. J. Med. 347, 322 (2002).

Taprostene CAS Registry Number: 108945-35-3 他前列烯

CAS Name: 3-[(Z)-[(3aR,4R,5R,6aS)-4-[(1E,3S)-3-Cyclohexyl-3-hydroxy-1-propenyl]hexahydro-5-hydroxy-2H-cyclopenta[b]furan-2-ylidene]methyl]benzoic acid
Additional Names: a-[(2Z,3aR,4R,5R,6aS)-4-...
Literature References: Prostacyclin analog; platelet aggregation inhibitor. Prepn: U. Seipp et al., EP 45842; eidem, US 4372971 (1982, 1983 both to Grünenthal); L. Flohé et al., Arzneim.-Forsch. 33, 1240 (1983). As adjuvant to thrombolytic therapy in acute myocardial infarction: F. W. Bär et al., Eur. Heart J. 14, 1118 (1993). Review of pharmacology and clinical experience: J. Schneider et al., Cardiovasc. Drug Rev. 11, 479-500 (1993).

Rosaprostol CAS Registry Number: 56695-65-9 罗沙前列醇

CAS Name: 2-Hexyl-5-hydroxycyclopentaneheptanoic acid
Additional Names: 9-hydroxy-19,20-bisnorprostanoic acidTrademarks: Rosal (IBI)
Percent Composition: C 72.44%, H 11.48%, O 16.08%
Literature References: Prostaglandin analog. Prepn, hypolipemic, platelet aggregation inhibitory activity: U. Valcavi, DE 2535343, eidem, US 4073938 (1976, 1978 both to Ist. Biochim. Ital.). Alternate process: V. Marotta, G. Zabban, EP 155392 (1985 to Ist. Biochim. Ital.). Gastric antisecretory, cytoprotective activity: U. Valcavi et al., Arzneim.-Forsch. 32, 657 (1982). Effect on mucus and gastrin secretion in duodenal ulcer: D. Foschi et al., Prostaglandins Leukotrienes Med. 15, 147 (1984). Comparison with cimetidine, q.v.: eidem, Drugs Exp. Clin. Res. 10, 427 (1984). Clinical evaluation in treatment of ulcers: G. P. Tincani et al., Minerva Med. 78, 847 (1987).

Latanoprost CAS Registry Number: 130209-82-4 拉坦前列素

CAS Name: (5Z)-7-[(1R,2R,3R,5S)-3,5-Dihydroxy-2-[(3R)-3-hydroxy-5-phenylpentyl]cyclopentyl]-5-heptenoic acid 1-methylethyl ester
Additional Names: isopropyl (Z)-7-[(1R,2R,3R,5S)-3,5-dihydroxy-2...
Literature References: Prostaglandin analog; prodrug of active acid metabolite. Prepd (not claimed): J. Ivanics et al., WO 9300329 (1993 to Kabi Pharmacia; Chinoin). Prepn: B. Resul et al., J. Med. Chem. 36, 243, 2242 (corr.) (1993). Clinical pharmacology: C. B. Toris et al., Ophthalmology 100, 1297 (1993). Clinical evaluation in glaucoma: P. Rácz et al., Arch. Ophthalmol. 111, 657 (1993); as single therapy and in combination with timolol, q.v.: A. H. Rulo et al., Br. J. Ophthalmol. 78, 899 (1994). Review of preclinical pharmacology: J. Stjernschantz et al., Adv. Prostaglandin Thromboxane Leukotriene Res. 23, 513-518 (1995).