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

Reproterol CAS Registry Number: 54063-54-6 瑞普特罗

CAS Name: 7-[3-[[2-(3,5-Dihydroxyphenyl)-2-hydroxyethyl]amino]propyl]-3,7-dihydro-1,3-dimethyl-1H-purine-2,6-dione
Additional Names: 7-[3-[(b,3,5-trihydroxyphenethyl)amino]propyl]theophyllinePe...
Literature References: Theophylline deriv which has selective activity on b2 receptors. Prepn: FR M5969 (1968 to Degussa), C.A. 71, 70644c (1969). See also FR Addn. 0308 (1970 to Degussa), C.A. 78, 72216h (1973). Synthesis: K. H. Klingler, Arzneim.-Forsch. 27, 4 (1977). Toxicology: S. Habersang, ibid. 45. Series of articles on metabolism, pharmacology and clinical trials: ibid. 15-76. Other clinical studies: D. Nolte et al., Dtsch. Med. Wochenschr. 102, 619 (1977); H. Budmiger et al., Schweiz. Med. Wochenschr. 108, 1190 (1978).

Xylidine CAS Registry Number: 1300-73-8 二甲基苯胺

CAS Name: ar,ar-Dimethylbenzenamine
Additional Names: dimethylaniline; aminodimethylbenzene
Percent Composition: C 79.29%, H 9.15%, N 11.56%
Literature References: There are six isomeric xylidines. Prepd by reduction of corresponding nitro-compounds: Allchin, US 1867962 (to I.C.I.); physical properties of all six isomers also given: Birch et al., J. Am. Chem. Soc. 71, 1362 (1949); van Loon et al., Rec. Trav. Chim. 79, 977 (1960); Bergmann, Berkovic, J. Org. Chem. 26, 919 (1961).

DBHBT CAS Registry Number: 63147-28-4

CAS Name: Mercaptoacetic acid [3,5-bis(1,1-dimethylethyl)-4-hydroxyphenyl]methyl ester
Additional Names: 3,5-di-tert-butyl-4-hydroxybenzylthioglycollate
Percent Composition: C 65.77%, H 8.44...
Literature References: Thermal stabilizer. Prepn: K. S. Cottman, US 4020042 (1977 to Goodyear); and stabilization of acrylonitrile-butadiene-styrene (ABS) terpolymer: E. G. Kolawole, J. B. Adeniyi, Eur. Polym. J. 18, 469 (1982). Stabilization of polystyrene and poly(methyl methacylate): E. G. Kolawole, J. Appl. Polym. Sci. 27, 3437 (1982); of Nigerian natural rubber: G. C. Ebi, E. G. Kolawole, ibid. 45, 2239 (1992).

Pyrithiamine CAS Registry Number: 534-64-5 吡啶硫胺氢溴酸盐

CAS Name: 1-[(4-Amino-2-methyl-5-pyrimidinyl)methyl]-3-(2-hydroxyethyl)-2-methylpyridinium bromide monohydrobromide
Additional Names: 1-(2-methyl-4-amino-5-pyrimidyl)methyl-2-methyl-3-hydroxyet...
Literature References: Thiamine antagonist prepd by condensation of 2-methyl-3-(b-hydroxyethyl)pyridine with the pyrimidine moiety of vitamin B1: Tracy, Elderfield, J. Org. Chem. 6, 54 (1941); improved procedure: Wilson, Harris, J. Am. Chem. Soc. 71, 2231 (1949); US 2587262 (1952 to Merck Co.). Cf. Woolley, J. Am. Chem. Soc. 72, 5763 (1950).

Acetylcysteine CAS Registry Number: 616-91-1 N-乙酰半胱氨酸

CAS Name: N-Acetyl-L-cysteine
Additional Names: L-a-acetamido-b-mercaptopropionic acid; N-acetyl-3-mercaptoalanine
Trademarks: Acetadote (Cumberland); Brunac (Bruschettini); Fabrol (Zyma); F...
Literature References: Thiol-containing antioxidant. Prepn: Smith, Gorin, J. Org. Chem. 26, 820 (1961). Prepn and use in treatment of respiratory diseases: Martin, Waller, US 3184505 (1965 to Mead Johnson). Effect in corneal healing: F. Menna et al., Bull. Mem. Soc. Fr. Opthalmol. 94, 425 (1982); G. Petroutsos et al., Ophthalmic Res. 14, 241 (1982). Toxicity: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Clinical trial in acetaminophen overdose: M. J. Smilkstein et al., N. Engl. J. Med. 319, 1557 (1988); as renal protectant with radiocontrast agents: M. Tepel et al., ibid. 343, 180 (2000). Review: G. R. McKinney, G. M. Sisson, in Pharmacological and Biochemical Properties of Drug Substances vol. 2, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1979) pp 479-488. Review of use in clinical toxicology: R. J. Flanagan, T. J. Meredith, Am. J. Med. 91, Suppl. 3C, 131S-139S (1991).

Lawesson's Reagent CAS Registry Number: 19172-47-5 劳森试剂

CAS Name: 2,4-Bis(4-methoxyphenyl)-1,3,2,4-dithiadiphosphetane 2,4-disulfide
Additional Names: anisyldithiophosphinic anhydride
Percent Composition: C 41.57%, H 3.49%, O 7.91%, P 15.32%, S 3...
Literature References: Thionating agent for conversion of carbonyls to thiocarbonyls. Prepn: H. Z. Lecher et al., J. Am. Chem. Soc. 78, 5018 (1956); and delineation of use: B. S. Pedersen et al., Bull. Soc. Chim. Belg. 87, 223 (1978); S. Scheibye et al., ibid., 229. Mechanistic study: T. B. Rauchfuss, G. A. Zank, Tetrahedron Lett. 27, 3445 (1986). Use in thionations: A. Z.-Q. Khan, J. Sandström, J. Chem. Soc. Perkin Trans. 1 1988, 2085; S. Araki et al., Bull. Chem. Soc. Jpn. 61, 2977 (1988); as reducing agent for sulfoxides: H. Bartsch, T. Erker, Tetrahedron Lett. 33, 199 (1992). Review of thionation reactions: M. P. Cava, M. I. Levinson, Tetrahedron 41, 5061-5087 (1985); of applications in organic and organometallic syntheses: M. Jesberger et al., Synthesis 2003, 1929-1958.

Clopenthixol CAS Registry Number: 982-24-1 氯哌噻吨

CAS Name: 4-[3-(2-Chloro-9H-thioxanthen-9-ylidene)propyl]-1-piperazineethanol
Additional Names: 2-chloro-9-[3-[4-(2-hydroxyethyl)-1-piperazinyl]propylidene]thiaxanthene
Percent Composition: ...
Literature References: Thioxanthene neuroleptic. Prepn (configuration not specified): BE 585338; P. V. Petersen et al., US 3116291 (1960, 1963 both to Kefalas A/S). Prepn of the pharmacologically active cis-isomer: BE 816855; N. Lassen, US 3996211 (1974, 1976 both to Kefalas A/S). Pharmacology: Cazzullo, Andreola, Acta Neurol. 20, 162 (1965); Weissman, Mod. Probl. Pharmacopsychiatry 2, 15 (1969); Moeller Nielsen, ibid. 23. Metabolism: Khan, Acta Pharmacol. Toxicol. 27, 202 (1969). HPLC determn of isomers in serum: T. Aaes-Jorgensen, J. Chromatogr. 188, 239 (1980). Series of articles on pharmacology and clinical studies: Acta Psychiatr. Scand. 64, Suppl. 294, 1-77 (1981).

Cefodizime CAS Registry Number: 69739-16-8 头孢地嗪酸

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-[[[5-(carboxymethyl)-4-methyl-2-thiazolyl]thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
...
Literature References: Third generation cephalosporin antibiotic with immunomodulating activity; derivative of cefotaxime, q.v. Prepn: BE 865632; W. Dürckheimer et al., US 4278793 (1978, 1981 both to Hoechst AG); and antibacterial activity: J. Blumbach et al., J. Antibiot. 40, 29 (1987). In vitro comparative antibacterial spectrum: R. N. Jones et al., Antimicrob. Agents Chemother. 20, 760 (1981); and b-lactamase stability: M. Limbert et al., J. Antibiot. 37, 892 (1984). In vivo antibacterial activity: N. Klesel et al., ibid. 1712. Enhancement of immune response in vivo: M. Limbert et al., ibid. 1719; and ex vivo: A. Fietta et al., Chemotherapy (Basel) 34, 430 (1988). HPLC determn in biological fluids: T. Marunaka et al., J. Chromatogr. 420, 329 (1987). Pharmacokinetics: N. Klesel et al., J. Antibiot. 37, 901 (1984); in humans: E. E. Dagrosa et al., Clin. Ther. 10, 18 (1987). Clinical study in urogenital gonorrhea: A. H. van der Willigen et al., Antimicrob. Agents Chemother. 32, 426 (1988). Physical properties, toxicology and structure-activity relationships: A. Bryskier et al., J. Antimicrob. Chemother. 26, Suppl. C, 1 (1990). Series of articles on pharmacology, pharmacokinetics and clinical studies: Chemotherapy (Tokyo) 36, Suppl. 5, 1-980 (1988); and immunomodulating activity: J. Antimicrob. Chemother. 26, Suppl. C, 1-134 (1990).

Ceftazidime CAS Registry Number: 72558-82-8 头孢他啶

CAS Name: 1-[[(6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)[(1-carboxy-1-methylethoxy)imino]acetyl]amino]-2-carboxy-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]pyridinium inner salt
Additiona...
Literature References: Third generation cephalosporin antibiotic. Prepn: C. H. O'Callaghan et al., DE 2921316; eidem, US 4258041 (1979, 1981 both to Glaxo). Prepn of crystalline pentahydrate: A. Brodie, L. A. Wetherill, DE 3037102; eidem, US 4329453 (1981, 1982 both to Glaxo). Chemical and antibacterial properties: eidem, Antimicrob. Agents Chemother. 17, 876 (1980). Activity vs Pseudomonas and Enterobacteriaceae: L. Verbist, J. Verhaegen, ibid. 807. In vitro comparison with other b-lactams: R. Wise et al., ibid. 884; L. Verbist, ibid. 19, 407 (1981). Symposium on clinical studies: J. Antimicrob. Chemother. 12, Suppl. A, 1-414 (1983). Review of antibacterial activity, pharmacokinetics and therapeutic use: D. M. Richards, R. N. Brogden, Drugs 29, 105-161 (1985). Comprehensive description: M. A. Abounassif et al., Anal. Profiles Drug Subs. 19, 95-121 (1990).

Cefsulodin CAS Registry Number: 62587-73-9 头孢磺啶

CAS Name: 4-(Aminocarbonyl)-1-[[(6R,7R)-2-carboxy-8-oxo-7-[[(2R)-phenylsulfoacetyl]amino]-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]pyridinium inner salt
Additional Names: 7-(a-sulphopheny...
Literature References: Third generation cephalosporin antibiotic. Prepn: S. Morimoto et al., DE 2234280; eidem, US 4065619 (1973, 1977 both to Takeda). Prepn and separation of isomers: H. Nomura et al., J. Med. Chem. 17, 1312 (1974). In vitro and in vivo antibacterial activity: K. Tsuchiya et al., Antimicrob. Agents Chemother. 13, 137 (1978). Absorption, distribution, excretion in mice, rats, dogs: eidem, J. Antibiot. 31, 593 (1978). Activity and susceptibility to b-lactamases: A. King et al., Antimicrob. Agents Chemother. 17, 165 (1980). In vitro comparison with other antibacterials: H. Grimm, Arzneim.-Forsch. 30, 1478 (1980). Clinical pharmacology: J. Fuellhaas et al., Curr. Chemother., Proc. 10th Int. Congr. Chemother. (Washington, D.C., 1978) 2, 848-851. Review of activity: H. C. Neu, B. E. Scully, Rev. Infect. Dis. 6, Suppl. 3, S667-S677 (1984). Review: A. Bryskier, Lyon Pharm. 34, 343-355 (1983); D. B. Wright, Drug Intell. Clin. Pharm. 20, 845-849 (1986).