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

Acetoxolone CAS Registry Number: 6277-14-1 乙酰甘草亭酸铝

CAS Name: (3b,20b)-3-(Acetyloxy)-11-oxoolean-12-en-29-oic acid
Additional Names: 3b-hydroxy-11-oxoolean-12-en-30-oic acid acetate; 3-O-acetyl-18b-glycyrrhetic acid; acetylglycyrrhetinic acid; g...
Literature References: Deriv of enoxolone, q.v.; homolog of carbenoxolone, q.v. Prepn: J. M. Beaton, F. S. Spring, J. Chem. Soc. 1955, 3126. Prepn of the aluminum salt: A. Bonati, ZA 7006901; idem, US 3764618 (1971, 1973 both to Dott. Inverni Della Beffa). NMR study of the acetate: M. Mousseron-Canet et al., Bull. Soc. Chim. Fr. 12, 4668 (1967). Pharmacology of the aluminum salt: C. Capra, Fitoterapia 40, 8 (1969), C.A. 73, 64754 (1970). Absorption in rats: B. D. Cameron et al., Arzneim.-Forsch. 26, 1680 (1976). Analysis of gastric protective effect: P. Altmayer et al., ibid. 31, 853 (1981).

Proglumetacin CAS Registry Number: 57132-53-3 普各洛美他辛

CAS Name: 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid 2-[4-[3-[[4-(benzoylamino)-5-(dipropylamino)-1,5-dioxopentyl]oxy]propyl]-1-piperazinyl]ethyl ester
Additional Names: (&#...
Literature References: Deriv of indomethacin, q.v. Prepn: F. Makovec et al., DE 2535799 corresp to US 3985878 (both 1976 to Rotta). Series of articles on pharmacology, mechanism of action, safety: Arzneim.-Forsch. 29, 1116-1129 (1979). Bioavailability study: A. A. Bignamini, P. L. Casula, Curr. Med. Res. Opin. 6, 299 (1979). Clinical evaluation: J. Münzenberg, S. Tachibana, Pharmatherapeutica 2, 279 (1980); P. Loizzi et al., ibid. 285. Mutagenicity study: R. Vidal y Plana et al., Farmaco Ed. Prat. 33, 543 (1978). Toxicity data for dimaleate: A. L. Rovati et al., Arzneim.-Forsch. 29, 1116 (1979).

Acemetacin CAS Registry Number: 53164-05-9 阿西美辛

CAS Name: 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid carboxymethyl ester
Additional Names: [[1-(4-chlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetoxy]acetic acidTrademarks: ...
Literature References: Deriv of indomethacin, q.v. Prepn: K. H. Boltze et al., DE 2234651; eidem, US 3910952 (1972, 1975 both to Troponwerke). Series of articles on chemistry, analysis, pharmacodynamics, toxicology and clinical trials: Arzneim.-Forsch. 30, 1313-1468 (1980). Toxicity data: H. Jacobi, H.-D. Dell, ibid. 1398.

Oxametacine CAS Registry Number: 27035-30-9 奥沙美辛

CAS Name: 1-(4-Chlorobenzoyl)-N-hydroxy-5-methoxy-2-methyl-1H-indole-3-acetamide
Additional Names: 1-(p-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetohydroxamic acid; indoxamic acid
Tradema...
Literature References: Deriv of indomethacin, q.v. Prepn: R. Aries, FR 1599495 (1969), C.A. 73, 3797h (1970); F. De Martiis et al., DE 2008332 corresp to US 3624103 (both 1971 to ABC); eidem, Boll. Chim. Farm. 114, 309 (1975). Pharmaco-toxicological evaluation: eidem, ibid. 319. Disposition in rats: L. F. Elsom et al., Arzneim.-Forsch. 29, 1155 (1979). Pharmacokinetics: P. Dittrich et al., ibid. 31, 518 (1981). Effect on prostaglandin biosynthesis: J. S. Franzone et al., Farmaco Ed. Sci. 35, 498 (1980). Clinical study: J. Polderman, M. Colon, J. Int. Med. Res. 8, 156 (1980).

Exalamide CAS Registry Number: 53370-90-4 依沙酰胺

CAS Name: 2-(Hexyloxy)benzamide
Additional Names: HBA
Trademarks: Hyperan (SS Pharm.)
Percent Composition: C 70.56%, H 8.65%, N 6.33%, O 14.46%
Literature References: Deriv of salicylamide, q.v. Prepn: E. M. Bevin et al., J. Pharm. Pharmacol. 4, 872 (1952); F. J. MacRae, D. E. Seymour, GB 726786 (1955 to Herts Pharm.), C.A. 50, 5751i (1956); L. V. Coates et al., J. Pharm. Pharmacol. 9, 855 (1957). Metabolism: Y. Kanaiwa et al., Yakugaku Zasshi 95, 411 (1975), C.A. 83, 71428v (1975). General pharmacologic effects: R. Inoki et al., Oyo Yakuri 10, 165 (1975), C.A. 88, 115369 (1976). Comparative study of antifungal efficacy vs clinical isolates: T. Kusunoki, S. Harada, J. Dermatol. 11, 227 (1984).

Ticarbodine CAS Registry Number: 31932-09-9 替卡波定

CAS Name: 2,6-Dimethyl-N-[3-(trifluoromethyl)phenyl]-1-piperidinecarbothioamide
Additional Names: a,a,a-trifluoro-2,6-dimethylthio-1-piperidinecarboxy-m-toluidideTrademarks: Tribodine (Elanco)<...
Literature References: Deriv of thiourea. Prepn: H. D. Porter, H. M. Taylor, US 3659012 (1972 to Lilly). Anthelmintic efficacy in dogs: R. J. Boisvenue et al., Am. J. Vet. Res. 33, 709 (1972); G. F. Slonka et al., ibid. 1075; D. K. Hass, J. A. Collins, Proc. Helminthol. Soc. Wash. 43, 135 (1976).

Cetraxate CAS Registry Number: 34675-84-8 西曲酸酯

CAS Name: 4-[[[trans-4-(Aminomethyl)cyclohexyl]carbonyl]oxy]benzenepropanoic acid
Additional Names: p-hydroxyhydrocinnamic acid trans-(4-aminomethyl)cyclohexanecarboxylate; tranexamic acid p-(2...
Literature References: Deriv of tranexamic acid, q.v. Prepn: Y. Yamamura et al., DE 1951061; eidem, US 3699149 (1970, 1972 both to Daiichi); O. Atsuji et al., J. Med. Chem. 15, 247 (1972); S. Kitahara, JP Kokai 73 75547 (1973 to Daiichi), C.A. 80, 59727x (1974). Mechanism of action: Y. Suzuki et al., Jpn. J. Pharmacol. 29, 829 (1979), C.A. 92, 88029 (1980). Anti-ulcer effects in rats: T. Hashizume et al., Arch. Int. Pharmacodyn. Ther. 240, 314 (1979). Clinical study: A. Ishimori et al., Arzneim.-Forsch. 29, 1625 (1979); S. Yamagata, K. Miura, ibid. 33, 1191 (1983).

Vinpocetine CAS Registry Number: 42971-09-5 长春西汀

CAS Name: (3a,16a)-Eburnamenine-14-carboxylic acid ethyl ester
Additional Names: 3a,16a-apovincaminic acid ethyl ester; ethyl apovincamin-22-oateTrademarks: Cavinton (Thiemann)
Percent Compo...
Literature References: Deriv of vincamine, q.v., with vasodilating activity. Prepn: C. Lörincz et al., DE 2253750; eidem, US 4035370 (1973, 1977 both to Gedeon Richter); eidem, Arzneim.-Forsch. 26, 1907 (1976). Series of articles on pharmacology, biochemistry, metabolism, pharmacokinetics, clinical studies: ibid. 1908-1989. Toxicity studies: E. Pálosi, L. Szporny, ibid. 1926; E. Cholnoky, L. I. Dömök, ibid. 1939. HPLC studies: G. Szepesi, M. Gazdag, J. Chromatogr. 205, 57, 341 (1981). Evaluation of effectiveness as antimotion drug: E. I. Matsnev, D. Bodo, Aviat. Space Environ. Med. 55, 281 (1984). One-pot synthesis from vincamine: Y. Kuge et al., Synth. Commun. 24, 759 (1994).

Dienogest CAS Registry Number: 65928-58-7 地诺孕素

CAS Name: (17a)-17-Hydroxy-3-oxo-19-norpregna-4,9-diene-21-nitrile
Additional Names: 17a-cyanomethyl-17b-hydroxy-13b-methylgona-4,9-dien-3-one; 17a-cyanomethyl-17b-hydroxy-4,9-estradien-3-one; ...
Literature References: Derivative of 19-nortestosterone. Prepn: K. Ponsold et al., DE 2718872; eidem, US 4167517 (1977, 1979 both to VEB Jenapharm); M. Hübner et al., Arzneim.-Forsch. 30, 401 (1980). Structure-activity study: M Hübner, K. Ponsold, Exp. Clin. Endocrinol. 81, 109 (1983). Evaluation of combination with estrogen as oral contraceptive: J. Spona et al., Contraception 56, 185 (1997); as hormone replacement therapy: T. Gräser et al., Maturitas 35, 253 (2000). Review of pharmacology and clinical experience: R. H. Foster, M. I. Wilde, Drugs 56, 825-833 (1998).

Artesunate CAS Registry Number: 88495-63-0 青蒿琥酯; 青蒿脂

CAS Name: Butanedioic acid mono[(3R,5aS,6R,8aS,9R,10R,12R,12aR)-decahydro-3,6,9-trimethyl-3,12-epoxy-12H-pyrano[4,3-j]-1,2-benzodioxepin-10-yl] ester
Additional Names: artesunic acid; dihydroqi...
Literature References: Derivative of artemisinin, q.v. Prepn: China Cooperative Research Group on Qinghaosu, J. Tradit. Chin. Med. 2, 9 (1982). Absolute configuration: X.-D. Luo et al., Helv. Chim. Acta 67, 1515 (1984). GC/MS determn.: A. D. Theoharides et al., Anal. Chem. 60, 115 (1988); HPLC determn in plasma: H. Naik et al., J. Chromatogr. B 816, 233 (2005). Pharmacology: Y. Zhao, J. Trop. Med. Hyg. 88, 391 (1985). Antimalarial activity: W. Peters et al., Ann. Trop. Med. Parasitol. 80, 483 (1986); A. J. Lin et al., J. Med. Chem. 30, 2147 (1987). Inhibition of cytochrome oxidase: Y. Zhao et al., J. Nat. Prod. 49, 139 (1986). Toxicology: China Cooperative Research Group on Qinghaosu, J. Tradit. Chin. Med. 2, 31 (1982). Series of articles on chemistry, pharmacology, and antimalarial efficacy: ibid. 3-50. Clinical trial as add-on therapy in pediatric malaria: L. von Seidlein et al., Lancet 355, 352 (2000). Review: R. N. Price, Expert Opin. Invest. Drugs 9, 1815-1827 (2000).