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

Cefazedone CAS Registry Number: 56187-47-4 头孢西酮

CAS Name: (6R,7R)-7-[[(3,5-Dichloro-4-oxo-1(4H)-pyridinyl)acetyl]amino]-3-[[(5-methyl-1,3,4-thiadiazol-2-yl)thio]methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional N...
Literature References: Semi-synthetic cephalosporin antibiotic. Prepn: R. Gerike et al., DE 2345402; eidem, US 4153693 (1975, 1979 both to E. Merck, W. Ger.). See also eidem, DE 2621011, DE 2626026, DE 2627204 (all 1977 to E. Merck, W. Ger.), C.A. 88, 5093, 105383, 121213 (1978). Series of articles on prepn, in vitro and in vivo activity, kinetics, pharmacology, toxicology, and clinical trials: Arzneim.-Forsch. 29, 361-462 (1979). Toxicity data: M. von Eberstein et al., ibid. 424.

Cefotiam CAS Registry Number: 61622-34-2 头孢替安

CAS Name: (6R,7R)-7-[[(2-Amino-4-thiazolyl)acetyl]amino]-3-[[[1-[2-(dimethylamino)ethyl]-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: Semi-synthetic cephalosporin antibiotic. Prepn: S. Terao et al., DE 2458695; M. Numata et al., US 4080498 (1975, 1978 both to Takeda); eidem, J. Antibiot. 31, 1262 (1978). Prepn of the crystalline dihydrochloride: K. Naito et al., DE 2738711; eidem, US 4146710 (1978, 1979 both to Takeda). Pharmacodynamics: K. Tsuchiya et al., ibid., 1272. Antibacterial spectrum: eidem, Antimicrob. Agents Chemother. 14, 557 (1978). Clinical trial in respiratory infections: H. M. Beumer et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 23, 105 (1985).

Quinupristin CAS Registry Number: 120138-50-3 奎奴普丁

CAS Name: 4-[4-(Dimethylamino)-N-methyl-L-phenylalanine]-5-[(2S,5R)-5-[[[(3S)-1-azabicyclo[2.2.2]oct-3-yl]thio]methyl]-4-oxo-2-piperidinecarboxylic acid]virginiamycin S1
Additional Names: 5d-[(...
Literature References: Semisynthetic depsipeptide type I streptogramin, q.v. Marketed in combination with dalfopristin, q.v. Prepn: J.-C. Barriere et al., EP 248703, eidem, US 4798827 (1987, 1989 both to Rhone-Poulenc). In vitro activity: H. C. Neu et al., J. Antimicrob. Chemother. 30, Suppl. A, 83 (1992). HPLC determn in plasma: A. Le Liboux et al., J. Chromatogr. B 708, 161 (1998).

Ivermectin CAS Registry Number: 70288-86-7

Additional Names: 22,23-Dihydroabamectin; 22,23-dihydroavermectin B1; 22,23-dihydro C-076B1Trademarks: Eqvalan (Merial); Heartgard 30 (Merial); Ivomec (Merial); Mectizan (Merck Co.); Noromectin (...
Literature References: Semi-synthetic deriv of abamectin, q.v., consists of a mixture of not less than 80% component B1a and not more than 20% component B1b. Prepn: JP Kokai 79 61198; J. C. Chabala, M. H. Fisher, US 4199569 (1979, 1980 both to Merck Co.); J. C. Chabala et al., J. Med. Chem. 23, 1134 (1980). Irreversible effects on adult parasites in onchocerciasis: A. P. Plaisier et al., J. Infect. Dis. 172, 204 (1995). Metabolism in animals: S.-H. L. Chiu et al., Drug Metab. Dispos. 14, 590 (1986). Pharmacokinetics in horses and sheep: S. E. Marriner et al., J. Vet. Pharmacol. Ther. 10, 175 (1987). HPLC determn in cattle and sheep tissues: P. C. Tway et al., J. Agric. Food Chem. 29, 1059 (1981); in human plasma and milk: R. Chiou et al., J. Chromatogr. 416, 196 (1987). Review of early chemistry and biology: W. C. Campbell et al., Science 221, 823-828 (1983). Review of clinical use and pharmacology: W. C. Campbell, G. W. Benz, J. Vet. Pharmacol. Ther. 7, 1-16 (1984); T. B. Barragry, Can. Vet. J. 28, 512-517 (1987); of pharmacology: J. L. Bennett et al., Parasitol. Today 4, 226-228 (1988). Book: Ivermectin and Abamectin, W. C. Campbell, Ed. (Springer-Verlag, New York, 1989) 363 pp. Review in filariasis: D. Richard-Lenoble et al., Fundam. Clin. Pharmacol. 17, 199-203 (2003). See also: Avermectins.

Talaporfin CAS Registry Number: 110230-98-3 他拉泊芬

CAS Name: N-[[(7S,8S)-3-Carboxy-7-(2-carboxyethyl)-13-ethenyl-18-ethyl-7,8-dihydro-2,8,12,17-tetramethyl-21H,23H-porphin-5-yl]acetyl]-L-aspartic acid
Additional Names: (2S,3S)-18-carboxy-20-[N-...
Literature References: Semisynthetic derivative of chlorin e6, q.v. Photosensitizer activated at 664 nm by laser or light-emitting diode-based light infusion device. Causes irreversible tumor blood vessel closure. Prepn: J. C. Bommer, B. F. Burnham, EP 168831; eidem, US 4675338 (1986, 1987 both to Nippon Petrochemicals). Photophysical properties: J. D. Spikes, J. C. Bommer, J. Photochem. Photobiol. B 17, 135 (1993); L. Li et al., ibid. 67, 51 (2002). Chemical and NMR structural studies: S. Gomi et al., Heterocycles 48, 2231 (1998). Safety assessment in treatment of refractory solid tumors: R. A. Lustig et al., Cancer 98, 1767 (2003). Clinical evaluation in lung cancer: H. Kato et al., Lung Cancer 42, 103 (2003).

Dirithromycin CAS Registry Number: 62013-04-1 地红霉素

CAS Name: (1R,2R,3R,6R,7S,8S,9R,10R,12R,13S,15R,17S)-7-[(2,6-Dideoxy-3-C-methyl-3-O-methyl-a-L-ribo-hexopyranosyl)oxy]-3-ethyl-2,10-dihydroxy-15-[(2-methoxyethoxy)methyl]-2,6,8,10,12,17-hexamethyl...
Literature References: Semi-synthetic derivative of erythromycin, q.v. Prepn: BE 840431 (1976 to Thomae); R. Maier et al., US 4048306 (1977 to Boehringer, Ing.). Synthesis, 1H- and 13C-NMR, and antimicrobial evaluation: F. T. Counter et al., Antimicrob. Agents Chemother. 35, 1116 (1991). X-ray structure determn: P. Luger, R. Maier, J. Cryst. Mol. Struct. 9, 329 (1979). HPLC determn in plasma: G. W. Whitaker, T. D. Lindstrom, J. Liq. Chromatogr. 11, 3011 (1988). Symposium on antibacterial activity, pharmacology, and clinical experience: J. Antimicrob. Chemother. 31, Suppl. C, 1-185 (1993).

Docetaxel CAS Registry Number: 114977-28-5 多烯紫杉醇;多西他赛

CAS Name: (aR,bS)-b-[[(1,1-Dimethylethoxy)carbonyl]amino]-a-hydroxybenzenepropanoic acid (2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodec...
Literature References: Semisynthetic derivative of paclitaxel, q.v., prepd using a natural precursor, 10-deacetylbaccatin III, extracted from the needles of the European yew tree, Taxus baccata L., Taxaceae. Antimitotic agent that promotes the assembly of microtubules and inhibits their depolymerization to free tubulin. Prepn: M. Colin et al., EP 253738; eidem, US 4814470 (1988, 1989 both to Rhône-Poulenc Sante); L. Mangatal et al., Tetrahedron 45, 4177 (1989). Synthesis of the side chain: J.-N. Denis et al., J. Org. Chem. 56, 6939 (1991). Structure-activity study: F. Guéritte-Voegelein et al., J. Med. Chem. 34, 992 (1991). Cytotoxic activity and mechanism of action: I. Ringel, S. B. Horwitz, J. Natl. Cancer Inst. 83, 288 (1991). In vivo antitumor activity: M.-C. Bissery et al., Cancer Res. 51, 4845 (1991). HPLC determn: J. C. Vergniol et al., J. Chromatogr. 582, 273 (1992). Clinical pharmacokinetics and toxicology: J.-M. Extra et al., Cancer Res. 53, 1037 (1993). Clinical trials in prostate cancer: I. F. Tannock et al., N. Engl. J. Med. 351, 1502 (2004); D. P. Petrylak et al., ibid. 1513. Symposium on clinical experience: Semin. Oncol. 27, Suppl. 3, 1-29 (2000). Review of mechanism of action and combination therapies: R. S. Herbst, F. R. Khuri, Cancer Treat. Rev. 29, 407-415 (2003); of clinical studies in non-small cell lung cancer: A. M. Davies et al., Expert Opin. Pharmacother. 4, 553-565 (2003).

Teniposide CAS Registry Number: 29767-20-2 替尼泊苷

CAS Name: (5R,5aR,8aR,9S)-5,8,8a,9-Tetrahydro-5-(4-hydroxy-3,5-dimethoxyphenyl)-9-[[4,6-O-[(R)-2-thienylmethylene]-b-D-glucopyranosyl]oxy]furo[3',4':6,7]naphtho[2,3-d]-1,3-dioxol-6(5aH)-one
Add...
Literature References: Semi-synthetic derivative of podophyllotoxin, q.v. Prepn: A. Von Wartburg, ZA 6607585; C. Keeler-Juslen et al., US 3524844 (1968, 1970 both to Sandoz). Mechanism of action: H. Stählen, Eur. J. Cancer 6, 303 (1970). Pharmacology: M. Hacker, D. Roberts, Cancer Res. 37, 3287 (1977); S. M. Sieber et al., Teratology 18, 31 (1978); T. J. Vietti et al., Cancer Treat. Rep. 62, 1313 (1978). Metabolism: L. Allen, Drug Metab. Rev. 8, 119 (1978); Cancer Res. 38, 2549 (1978). Clinical studies: N. M. Gadel-Mawla et al., Cancer Treat. Rep. 62, 993 (1978); R. E. Bellet et al., ibid. 445. Studies on delayed toxicity in mice after i.p. injections: M. Hacker, D. Roberts, Cancer Res. 35, 1756 (1975); H. Stählin, Eur. J. Cancer 12, 925 (1976). Review of pharmacology, pharmacokinetics and assay methods: P. I. Clark, M. L. Slevin, Clin. Pharmacokinet. 12, 223-252 (1987). Comprehensive description: J. J. Kettenes-van den Bosch et al., Anal. Profiles Drug Subs. 19, 575-600 (1990).

Rifabutin CAS Registry Number: 72559-06-9 利福布汀

CAS Name: 1',4-Didehydro-1-deoxy-1,4-dihydro-5'-(2-methylpropyl)-1-oxorifamycin XIV
Additional Names: (9S,12E,14S,15R,16S,17R,18R,19R,20S,21S,22E,24Z)-6,16,18,20-tetrahydroxy-1'-isobutyl-14-met...
Literature References: Semisynthetic derivative of rifamycin S that inhibits nucleic acid synthesis. Prepn: L. Marsili et al., DE 2825445 (1979 to Farmitalia); eidem, US 4219478 (1980 to Archifar Labs). In vitro and in vivo antibacterial activity: A. Sanfilippo et al., J. Antibiot. 33, 1193 (1980); C. Della Bruna et al., ibid. 36, 1502 (1983). Mechanism of action: D. Ungheri et al., Drugs Exp. Clin. Res. 10, 681 (1984). Comparative in vitro antimycobacterial spectrum: J. M. Dickinson, D. A. Mitchison, Tubercle 68, 177 (1987). In vitro inhibition of HIV-1 replication: R. Anand et al., Antimicrob. Agents Chemother. 32, 684 (1988). Clinical pharmacokinetics: M. H. Skinner et al., ibid. 33, 1237 (1989). Pharmacology and clinical efficacy in mycobacterial infections: R. J. O'Brien et al., Rev. Infect. Dis. 9, 519 (1987).

Rifalazil CAS Registry Number: 129791-92-0 利福拉齐

CAS Name: 1',4-Didehydro-1-deoxy-1,4-dihydro-3'-hydroxy-5'-[4-(2-methylpropyl)-1-piperazinyl]-1-oxorifamycin VIII
Additional Names: (2S,16Z,18E,20S,21S,22R,23R,24R,25S,26R,27S,28E)-5,12,21,23,2...
Literature References: Semisynthetic derivative of rifamycin S, q.v. Prepn: T. Yamane et al., EP 366914; eidem, US 4983602 (1990, 1991 both to Kanegafuchi); eidem, Chem. Pharm. Bull. 41, 148 (1993). Antimycobacterial efficacy in comparison with rifampin, q.v.: T. Yamamoto et al., Antimicrob. Agents Chemother. 40, 426 (1996). Pharmacokinetics: K. Hosoe et al., ibid. 2749. HPLC determn in biological fluids: eidem, J. Chromatogr. B 653, 177 (1994). Review of pharmacology and clinical studies: D. M. Rothstein et al., Expert Opin. Invest. Drugs 12, 255-271 (2003).