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

Bietaserpine CAS Registry Number: 53-18-9 比他舍平

CAS Name: (3b,16b,17a,18b,20a)-1-[2-(Diethylamino)ethyl]-11,17-dimethoxy-18-[(3,4,5-trimethoxybenzoyl)oxy]yohimban-16-carboxylic acid methyl ester
Additional Names: 1-[2-(diethylamino)ethyl]-18...
Literature References: Prepn: Buzas, Régnier, C.R. Hebd. Seances Acad. Sci. 250, 1340 (1960); Buzas et al., FR 1256524 (1961 to Dautreville Lebas and Andre Buzas), C.A. 57, 2273e (1962); Buzas et al., FR M102 C.A. 58, 9159a (1963); GB 894866 (1961, 1962 both to Soc. Nogentaise de Prods. Chim. and Andre Buzas). Pharmacology: Garattini et al., J. Pharm. Pharmacol. 13, 548 (1961); Quevauviller et al., Therapie 18, 1429 (1963); Guerrin et al., C.R. Seances Soc. Biol. Ses Fil. 158, 1096 (1964); P. Berthaux, M. Neuman, Arzneim.-Forsch. 14, 1040 (1964).

Oxfendazole CAS Registry Number: 53716-50-0 奥芬达唑

CAS Name: [5-(Phenylsulfinyl)-1H-benzimidazol-2-yl]carbamic acid methyl ester
Additional Names: methyl-5-(phenylsulfinyl)-2-benzimidazolecarbamate; 5-phenylsulfinyl-2-carbomethoxyaminobenzimida...
Literature References: Prepn: C. Beard et al., DE 2363351; eidem, US 3929821 (1974, 1975, both to Syntex); E. A. Averkin et al., J. Med. Chem. 18, 1164 (1975). Metabolism: J. P. Bell, R. V. Tomlinson, Fed. Proc. 35, 487 (1976). Radioimmunoassay: C. Nerenberg et al., J. Pharm. Sci. 67, 1553 (1978). Efficacy evaluations: J. L. Duncan, J. G. Reid, Vet. Rec. 103, 332 (1978); N. F. Baker et al., Am. J. Vet. Res. 39, 1258 (1978).

Triamcinolone Benetonide CAS Registry Number: 31002-79-6 苯曲安奈德

CAS Name: (11b,16a)-21-[3-(Benzoylamino)-2-methyl-1-oxopropoxy]-9-fluoro-11-hydroxy-16,17-[(1-methylethylidene)bis(oxy)]pregna-1,4-diene-3,20-dione
Additional Names: 9-fluoro-11b,16a,17,21-tetr...
Literature References: Prepn: C. Cavazza et al., DE 2047218; eidem, US 3749712 (1971, 1973 both to Sigma-Tau). Pharmacology: E. T. Ordonez, Arzneim.-Forsch. 21, 248 (1971). Percutaneous absorption by rats and rabbits: W. H. Down et al., Toxicol. Lett. 1, 95 (1977). Clinical study: D. J. Tazelaar, J. Int. Med. Res. 5, 338 (1977). HPLC analysis: S. Muck et al., Boll. Chim. Farm. 120, 240 (1981). For structure see Triamcinolone Acetonide.

Esaprazole CAS Registry Number: 64204-55-3 艾沙拉唑

CAS Name: N-Cyclohexyl-1-piperazineacetamide
Additional Names: 1-piperazinyl-4-methylenecarbonylcyclohexylamine; N-(1-piperazinylacetyl)cyclohexylamine; N-[(N-cyclohexylcarbamoyl)methyl]piperaz...
Literature References: Prepn: C. Corvi-Mora, DE 2702537; idem, US 4123530 (1977, 1978 both to Camillo Corvi). Metabolism in animals and man: P. Ventura et al., Farmaco Ed. Prat. 39, 190 (1984). Cytoprotective activity: B. Lumachi, R. Scuri, Drugs Exp. Clin. Res. 11, 693 (1985); and pharmacology: R. Scuri et al., Boll. Chim. Farm. 123, 425 (1983). Pharmacology: G. Coruzzi et al., Farmaco Ed. Prat. 40, 313 (1985); G. Coruzzi et al., ibid. 324. Antisecretory activity in humans: L. Erembourg et al., Int. J. Clin. Pharmacol. Res. 7, 95 (1987). HPLC determn in biological fluids: M. A. Girometta et al., J. Chromatogr. 383, 85 (1986). Clinical trial in comparison with cimetidine: L. Capurso et al., Clin. Trials J. 23, 293 (1986).

Doxapram CAS Registry Number: 309-29-5 多沙普仑

CAS Name: 1-Ethyl-4-[2-(4-morpholinyl)ethyl]-3,3-diphenyl-2-pyrrolidinone
Percent Composition: C 76.16%, H 7.99%, N 7.40%, O 8.45%
Literature References: Prepn: C. D. Lunsford, A. D. Cale, BE 613734; eidem, US 3192206 (1962, 1965 both to A. H. Robins); Lunsford et al., J. Med. Chem. 7, 302 (1964). Clinical comparison with mepixanox in chronic bronchopulmonary disease: M. Parziale et al., G. Ital. Mal. Torace 38, 323 (1984). Toxicity data: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971).

Aspirin CAS Registry Number: 50-78-2 阿司匹林

CAS Name: 2-(Acetyloxy)benzoic acid
Additional Names: salicylic acid acetate; 2-acetoxybenzoic acid; acetylsalicylic acid
Trademarks: Acylpyrin (Slovakofarma); Angettes (BMS); Asatard (Boehr...
Literature References: Prepn: C. Gerhardt, Ann. 87, 149 (1853). Manuf from salicylic acid and acetic anhydride: Faith, Keyes Clark's Industrial Chemicals, F. A. Lowenheim, M. K. Moran, Eds. (Wiley-Interscience, New York, 4th ed., 1975) pp 117-120. Crystallization from acetone: Hamer, Phillips, US 2890240 (1959 to Monsanto). Novel process involving distillation: Edmunds, US 3235583 (1966 to Norwich Pharm.). Crystal structure: P. J. Wheatley, J. Chem. Soc. (Suppl.) 1964, 6036. Characterization of a second polymorphic form: P. Vishweshwar et al., J. Am. Chem. Soc. 127, 16802 (2005). Toxicity data: E. R. Hart, J. Pharmacol. Exp. Ther. 89, 205 (1947). Evaluation as a risk factor in Reye's syndrome: P. J. Waldman et al., J. Am. Med. Assoc. 247, 3089 (1982). Review of clinical trials in prevention of myocardial infarction and stroke: P. C. Elwood, Drugs 28, 1-5 (1984). Symposium on aspirin therapy: Am. J. Med. 74, no. 6A, 1-109 (1983). Clinical trials in prevention of colorectal cancer: R. S. Sandler et al., N. Engl. J. Med. 348, 883 (2003); J. A. Baron et al., ibid. 891. Comprehensive description: K. Florey, Anal. Profiles Drug Subs. 8, 1-46 (1979). Monograph: M. J. H. Smith, P. K. Smith, The Salicylates (Interscience, New York, 1966) 313 pp. Book: Acetylsalicylic Acid, H. J. M. Barnett et al., Eds. (Raven, New York, 1982) 278 pp.

Doxylamine CAS Registry Number: 469-21-6 多西拉敏

CAS Name: N,N-Dimethyl-2-[1-phenyl-1-(2-pyridinyl)ethoxy]ethanamine
Additional Names: 2-[a-(2-dimethylaminoethoxy)-a-methylbenzyl]pyridine; phenyl-2-pyridylmethyl-b-N,N-dimethylaminoethyl ether...
Literature References: Prepn: C. H. Tilford et al., J. Am. Chem. Soc. 70, 4001 (1948); N. Sperber et al., ibid. 71, 887 (1949). Pharmacology: B. B. Brown, H. Werner, J. Lab. Clin. Med. 33, 325 (1948). GC determn: H. C. Thompson et al., J. Chromatogr. Sci. 20, 373 (1982). Chronic toxicity study: C. D. Jackson, B. Blackwell, J. Am. Coll. Toxicol. 12, 1 (1993). Review of properties and pharmacology: T. J. Haley, Dangerous Prop. Ind. Mater. Rep. 2, 17-20 (1982). Clinical evaluation as hypnotic: F. Sjöqvist, L. Lasagna, Clin. Pharmacol. Ther. 8, 48 (1967); as antihistaminic for use in colds: R. Eccles et al., J. Pharm. Pharmacol. 47, 990 (1995).

Trifluridine CAS Registry Number: 70-00-8 曲氟尿苷

CAS Name: a,a,a-Trifluorothymidine
Additional Names: 2'-deoxy-5-(trifluoromethyl)uridine; 5-(trifluoromethyl)-2'-deoxyuridine; F3TDRTrademarks: TFT Thilo (Alcon-Thilo); Virophta (Dulcis); Virop...
Literature References: Prepn: C. Heidelberger et al., J. Am. Chem. Soc. 84, 3597 (1962); eidem, J. Med. Chem. 7, 1 (1964); C. Heidelberger, US 3201387 (1965 to U.S. Dept. HEW). Crystal structure: A. H. Tench, Diss. Abstr. Int. B 33, 3587 (1973). NMR study: R. J. Cushley et al., J. Am. Chem. Soc. 90, 709 (1968). Metabolism: D. L. Dexter et al., Cancer Res. 32, 247 (1972); W. J. O'Brien, H. F. Edelhauser, Invest. Ophthalmol. Visual Sci. 16, 1093 (1977). Pharmacodynamics: B. L. Wigdahl, J. R. Parkhurst, Antimicrob. Agents Chemother. 14, 470 (1978); G. J. Smith et al., Biochem. Biophys. Res. Commun. 83, 1538 (1978). Teratogenicity study: M. Itoi et al., Arch. Ophthalmol. 93, 46 (1975). Cytotoxicity and mutagenicity study: E. Huberman, C. Heidelberger, Mutat. Res. 14, 130 (1972). Clinical studies: H. E. Kaufman, Invest. Ophthalmol. Visual Sci. 17, 941 (1978); R. A. Hyndiuk et al., Arch. Ophthalmol. 96, 1839 (1978). Review of mechanism of antiviral activity: C. Heidelberger, Ann. N.Y. Acad. Sci. 255, 317 (1975). Review of pharmacology and therapeutic use: A. A. Carmine et al., Drugs 23, 329-353 (1982).

Benzoquinonium Chloride CAS Registry Number: 311-09-1

CAS Name: N,N'-[(3,6-Dioxo-1,4-cyclohexadiene-1,4-diyl)bis(imino-3,1-propanediyl)]bis[N,N-diethylbenzenemethanaminium]dichloride
Additional Names: [2,5-p-benzoquinonylenebis(iminotrimethylene)]...
Literature References: Prepn: C. J. Cavallito et al., J. Am. Chem. Soc. 72, 2661 (1950); C. J. Cavallito, US 2844585 (1958 to Sterling).

Clomacran CAS Registry Number: 5310-55-4 氯马克仑

CAS Name: 2-Chloro-9,10-dihydro-N,N-dimethyl-9-acridinepropanamine
Additional Names: 2-chloro-9-[3-(dimethylamino)propyl]acridanPercent Composition: C 71.87%, H 7.04%, Cl 11.79%, N 9.31%
Literature References: Prepn: C. L. Zirkle, US 3131190 (1964 to SKF). Effect on in vivo histamine metabolism: R. Schayer, M. A. Reilly, Arch. Int. Pharmacodyn. Ther. 203, 123 (1973). Clinical potency in relation to dopamine-binding: P. Seeman et al., Nature 261, 717 (1976). Pharmacology: P. Fowler et al., Arzneim.-Forsch. 27, 866 (1977). Photooxidation study: W. R. Knappe, J. Pharm. Sci. 67, 318 (1978).