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

Cefmenoxime CAS Registry Number: 65085-01-0 头孢甲肟

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-[[(1-methyl-1H-tetrazol-5-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Na...
Literature References: Third generation cephalosporin antibiotic; related structurally to cefotaxime and ceftizoxime, q.q.v. The name cefmenoxime applies to the isomer having a syn-methoxyimino group. Prepn (unspecified stereochemistry): M. Ochiai et al., DE 2556736; eidem, US 4098888 (1976, 1978 both to Takeda); syn-isomer: R. Heymes, A. Lutz, DE 2713272; eidem, US 4476122 (1983, 1984 both to Roussel-Uclaf). Series of articles on antibacterial activity, absorption, excretion, metabolism, mechanism of action, clinical studies: Chemotherapy (Tokyo) 29, Suppl. 1, 1-998 (1979). In vitro and in vivo study: K. Tsuchiya et al., Antimicrob. Agents Chemother. 19, 56 (1981). b-Lactamase stability: K. Okonogi et al., ibid. 20, 171 (1981). Clinical pharmacokinetics study: D. Höffler, P. Koeppe, Arzneim.-Forsch. 33, 269 (1983). Symposium: Am. J. Med. 77(6A), 1-59 (1984).

Gemifloxacin CAS Registry Number: 175463-14-6 吉米沙星

CAS Name: 7-[3-(Aminomethyl)-4-(methoxyimino)-1-pyrrolidinyl]-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acidPercent Composition: C 55.52%, H 5.18%, F 4.88%, N 17.99%,...
Literature References: Third generation fluorinated quinolone antibacterial. Prepn: J. H. Kwak et al., EP 688772; C. Y. Hong et al., US 5633262 (1995, 1997 both to LG Chemical); C. Y. Hong et al., J. Med. Chem. 40, 3584 (1997). Antibacterial spectrum in vitro: R. Wise, J. M. Andrews, J. Antimicrob. Chemother. 44, 679 (1999). HPLC-tandem MS determn in human plasma: E. Doyle et al., J. Chromatogr. B 746, 191 (2000). Clinical pharmacokinetics: A. Allen et al., Antimicrob. Agents Chemother. 44, 1604 (2000). Review of antibacterial activity, pharmacology, and clinical trials: J. M. Blondeau, B. Missaghi, Expert Opin. Pharmacother. 5, 1117-1152 (2004).

Cefpimizole CAS Registry Number: 84880-03-5 头孢咪唑

CAS Name: 1-[[(6R,7R)-2-Carboxy-7-[[(2R)-[[(5-carboxy-1H-imidazol-4-yl)carbonyl]amino]phenylacetyl]amino]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-en-3-yl]methyl]-4-(2-sulfoethyl)pyridinium inner sal...
Literature References: Third generation injectable cephalosporin antibiotic. Prepn: N. Yasuda et al., DE 2826546; eidem, US 4217450 (1979, 1980 both to Ajinomoto); N. Yasuda et al., J. Antibiot. 36, 242 (1983). In vitro antibacterial activity and b-lactamase stability: H. C. Neu, P. Labthavikul, Antimicrob. Agents Chemother. 24, 375 (1983). Potentiating effect on phagocyte functions: H. Ohnishi et al., ibid. 23, 874 (1983). Toxicity study: S. Hashimoto et al., Toxicol. Lett. 23, 135 (1984). Therapeutic efficacy in mice: Y. Obana et al., J. Antimicrob. Chemother. 16, 727 (1985). HPLC determn in human plasma and urine: D. B. Lakings, J. M. Wozniak, J. Chromatogr. 308, 261 (1984). Pharmacokinetics in humans: D. B. Lakings et al., Antimicrob. Agents Chemother. 29, 271 (1986). Efficacy and tolerance in gonorrhea in men: E. T. Sandberg et al., ibid. 849.

Oxaliplatin CAS Registry Number: 61825-94-3 奥沙利铂

CAS Name: (SP-4-2)-[(1R,2R)-1,2-Cyclohexanediamine-kN,kN'][ethanedioato(2-)-kO1,kO2]platinum
Additional Names: [(1R,2R)-1,2-cyclohexanediamine-N,N'][oxalato (2-)-O,O']platinum; oxalato (1R,2R-c...
Literature References: Third generation platinum complex. Prepn and antitumor activity: Y. Kidani et al., J. Med. Chem. 21, 1315 (1978); Y. Kidani et al., Gann 71, 637 (1980). Crystal structure: M. A. Bruck et al., Inorg. Chim. Acta 92, 279 (1984). FAB and LAMMA MS analysis: J. Claereboudt et al., J. Pharm. Biomed. Anal. 7, 1599 (1989). Pharmacokinetics: R. Kizu et al., Cancer Chemother. Pharmacol. 31, 475 (1993). Clinical evaluation in colorectal cancer: F. Levi et al., Eur. J. Cancer 29A, 1280 (1993). Brief review of antitumor and clinical activity: G. Mathé et al., Biomed. Pharmacother. 43, 237-250 (1989). Review of clinical experience in combination therapy for colorectal cancer: D. Simpson et al., Drugs 63, 2127-2156 (2003).

Bifenthrin CAS Registry Number: 82657-04-3 氟氯菊酯

CAS Name: [1a,3a(Z)]-(±)-3-(2-Chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethylcyclopropanecarboxylic acid (2-methyl[1,1'-biphenyl]-3-yl)methyl ester
Additional Names: 2-methylbiphenyl-3-ylm...
Literature References: Third generation synthetic pyrethroid. Prepn: J. F. Engel, EP 3336; idem, US 4238505 (1979, 1980 both to FMC); E. L. Plummer et al., Pestic. Sci. 14, 560 (1983). Physical properties, toxicology and review of field studies: H. J. H. Doel et al., Meded. Fac. Landbouwwet. Rijksuniv. Gent 49, 929 (1984). Insecticidal activity: M. S. Mulla, H. A. Darwazeh, Bull. Soc. Vector Ecol. 10, 1 (1985); M. S. Hamed, C. O. Knowles, J. Econ. Entomol. 81, 1295 (1988). Field studies: Y. Antignus et al., Ann. Appl. Biol. 110, 557 (1987); J. T. Trumble et al., J. Econ. Entomol. 81, 608 (1988). Review of toxicology and human exposure: Toxicological Profile for Pyrethrins and Pyrethroids (PB2004-100004, 2003) 332 pp.

Cefteram CAS Registry Number: 82547-58-8 头孢特仑新戊酯

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)(methoxyimino)acetyl]amino]-3-[(5-methyl-2H-tetrazol-2-yl)methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: (...
Literature References: Third generation, orally active cephalosporin antibiotic. Prepn: BE 890499; H. Sadaki et al., US 4489072 (1982, 1984 both to Toyama). In vitro antibacterial activity: R. Wise et al., Antimicrob. Agents Chemother. 29, 1067 (1986); in vitro activity vs Neisseria gonorrhoeae: W. R. Bowie et al., ibid. 31, 470 (1987). General pharmacology in animals: S. Hirai et al., Jpn. J. Antibiot. 39, 958 (1986), C.A. 105, 183450a (1986). Pharmacokinetics and tissue distribution in animals: I. Saikawa et al., ibid. 979, C.A. 105, 183338v (1986). Series of articles on activity, toxicology, pharmacology and clinical efficacy: Chemotherapy (Tokyo) 34, Suppl. 2, 1-984 (1986). Acute toxicity: S. Sato et al., ibid. 166.

Picoplatin CAS Registry Number: 181630-15-9 甲啶铂,吡铂

CAS Name: (SP-4-3)-Amminedichloro(2-methylpyridine)platinum
Additional Names: cis-amminedichloro(2-methylpyridine)platinum(II)Percent Composition: C 19.16%, H 2.68%, Cl 18.85%, N 7.45%, Pt 51.8...
Literature References: Third generation, sterically hindered Pt-complex that exhibits reduced reactivity with sulfur ligands such as glutathione, q.v.; designed to overcome acquired Pt-chemotherapy resistance. Prepn: B. A. Murrer, EP 727430 (1996 to AnorMED; Inst. of Cancer Research); idem, US 5665771 (1997 to Johnson Matthey). Pharmacology and pharmacokinetics: F. I. Raynaud et al., Clin. Cancer Res. 3, 2063 (1997). Cytotoxicity and DNA binding activity: J. Holford et al., Anti-Cancer Drug Design 13, 1 (1998). In vitro circumvention of cisplatin resistance: idem, et al,. Br. J. Cancer 77, 366 (1998); of radiosensitizing activity: G. P. Raaphorst et al., Anticancer Res. 24, 613 (2004). LC/MS determn in plasma: T. Oe et al., Anal. Chem. 74, 591 (2002); in urine: eidem, J. Chromatogr. B 792, 217 (2003). Series of articles on clinical evaluations: Eur. J. Cancer 38, Suppl. S1-S31 (2002). Review of early development: L. R. Kelland et al., J. Inorg. Biochem. 77, 111-115 (1999); and therapeutic potential: M. P. Hay, Curr. Opin. Invest. Drugs 1, 263-266 (2000).

Isopilosine CAS Registry Number: 491-88-3 异毛果芸香素

CAS Name: (3S,4R)-Dihydro-3-[(R)-hydroxyphenylmethyl]-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone
Additional Names: carpiline; carpidine
Percent Composition: C 67.12%, H 6.34%, N 9....
Literature References: This compound was originally called pilosine (the cis-isomer of isopilosine): H. W. Voigtländer, W. Rosenberg, Arch. Pharm. 292, 579 (1959). Isoln from leaves of Pilocarpus microphyllus Stapf, Rutaceae: F. L. Pyman, J. Chem. Soc. 101, 2260 (1912). Synthesis and abs config: Link, Bernauer, Helv. Chim. Acta 55, 1053 (1972). Crystal structure: W. E. Oberhaensli, Cryst. Struct. Commun. 1, 203 (1972).

Graphitic Acid CAS Registry Number: 1399-57-1

Additional Names: Graphite oxide; graphitic oxide
Literature References: This material, obtained by oxidation of graphite, was first prepd by Brodie in 1859; Hummers, Offeman, J. Am. Chem. Soc. 80, 1339 (1958). Its composition is not well defined but usually given as C4O(OH): Aragon de la Cruz, Cowley, Nature 196, 468 (1962), Acta Crystallogr. 16, 531 (1963). Prepn and manufacture: Hummers, US 2798878 (1957 to National Lead); Hummers, Offeman, loc. cit.; Ruskin, US 2933381 and US 2944881 (both 1960 to Union Carbide). Crystal structure: Aragon de la Cruz, Cowley, loc. cit.

Glycerophosphoric Acid CAS Registry Number: 57-03-4 ( DL - a -form); 17181-54-3 ( b -form)

Additional Names: Phosphoric acid glycerol esters
Percent Composition: C 20.94%, H 5.27%, O 55.79%, P 18.00%
Literature References: Three isomers exist: b-glycerophosphoric acid, the D(+)- and L(-)-forms of a-glycerophosphoric acid. The L-a-acid is the naturally occurring form; the b-acid, present in hydrolyzates of lecithins from natural sources, arises from migration of the phosphoryl group from the a-carbon atom. See review: Dawson, Annu. Rep. Prog. Chem. 55, 365 (1958). Prepn by phosphorylation of glycerol results in a mixture of the a- and b-acids: Cherbuliez, Weniger, Helv. Chim. Acta 29, 2006 (1946). Prepn and configuration of L-a-acid: Baer, Fischer, J. Biol. Chem. 128, 491 (1939). Prepn of D-a-acid: eidem, ibid. 135, 321 (1940). Separation of a-acid from b- and polyglycerophosphoric acids: Carrara, IT 460219 (1950), C.A. 46, 5077a (1952).