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

Terbinafine CAS Registry Number: 91161-71-6 特比萘芬

CAS Name: N-[(2E)-6,6-Dimethyl-2-hepten-4-ynyl]-N-methyl-1-naphthalenemethanamine
Additional Names: trans-N-methyl-N-(1-naphthylmethyl)-6,6-dimethylhept-2-en-4-ynyl-1-amine
Percent Compositi...
Literature References: Orally active, antimycotic allylamine related to naftifine, q.v. Specific inhibitor of squalene epoxidase, a key enzyme in fungal ergosterol biosynthesis. Prepn: A. Stütz, EP 24587; idem, US 4755534 (1981, 1988 both to Sandoz); A. Stütz, G. Petranyi, J. Med. Chem. 27, 1539 (1984). Mode of action: G. Petranyi et al., Science 224, 1239 (1984); N. S. Ryder, Antimicrob. Agents Chemother. 27, 252 (1985). In vitro antifungal activity: S. Shadomy et al., Sabouraudia 23, 125 (1985). Toxicity data: U. Ganzinger et al., Proc. 13th Int. Congr. Chemother. 6, 116/52 (1983). Symposium on pharmacology and clinical trials: J. Am. Acad. Dermatol. 23, Suppl., 775-812 (1990). Clinical trial as systemic treatment of toenail onychomycosis: E. G. V. Evans et al., Br. Med. J. 318, 1031 (1999).

Faropenem CAS Registry Number: 106560-14-9 法罗培南钠

CAS Name: (5R,6S)-6-[(1R)-1-Hydroxyethyl]-7-oxo-3-[(2R)-tetrahydro-2-furanyl]-4-thia-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylic acid
Additional Names: fropenem; (5R,6S,8R,2'R)-2-(2'-tetrahydrof...
Literature References: Orally active, b-lactamase stable, penem antibiotic. Prepn: M. Ishiguro et al., EP 199446; eidem, US 4997829 (1986, 1991 both to Suntory); eidem, J. Antibiot. 41, 1685 (1988). Pharmacokinetics: A. Tsuji et al., Drug Metab. Dispos. 18, 245 (1990). In vitro antimicrobial spectrum: J. M. Woodcock et al., J. Antimicrob. Chemother. 39, 35 (1997). b-Lactamase stability: A. Dalhoff et al., Chemotherapy (Basel) 49, 229 (2003). HPLC determn in plasma: R. V. S. Nirogi et al., Arzneim.-Forsch. 55, 762 (2005). Clinical trial in urinary tract infections: S. Arakawa et al., Nishinihon J. Urol. 56, 300 (1994); in bacterial sinusitis: R. Siegert et al., Eur. Arch. Otorhinolaryngol. 260, 186 (2003).

Camostat CAS Registry Number: 59721-28-7 卡莫司他

CAS Name: 4-[[4-[(Aminoiminomethyl)amino]benzoyl]oxy]benzeneacetic acid 2-(dimethylamino)-2-oxoethyl ester
Additional Names: N,N-dimethylcarbamoylmethyl-p-(p-guanidinobenzoyloxy)phenylacetate Literature References: Orally active, non-peptide proteolytic enzyme inhibitor with anti-trypsin and anti-plasmin activities, related structurally to gabexate, q.v. Prepn: S. Fujii et al., DE 2548886; eidem, US 4021472 (1976, 1977 both to Ono). Enzyme inhibition study: Y. Tamura et al., Biochim. Biophys. Acta 484, 417 (1977). Inhibition of exptl tumors in mice: M. Ohkoshi, Gann 72, 959 (1981), C.A. 96, 97304v (1982); M. Ohkoshi, S. Fujii, ibid. 73, 108 (1982), C.A. 96, 155182s (1982). Prevention of acute exptl pancreatitis: S. Takasugi et al., Digestion 24, 36 (1982). Absorption and excretion: S. Hiraku et al., Iyakuhin Kenkyu 13, 756 (1982), C.A. 97, 120038t (1982).

Vardenafil CAS Registry Number: 224785-90-4 伐地那非

CAS Name: 1-[[3-(1,4-Dihydro-5-methyl-4-oxo-7-propylimidazo[5,1-f][1,2,4]triazin-2-yl)-4-ethoxyphenyl]sulfonyl]-4-ethyl-piperazine
Percent Composition: C 56.54%, H 6.60%, N 17.20%, O 13.10%, S ...
Literature References: Orally active, selective phosphodiesterase type 5 (PDE5) inhibitor. Prepn: U. Niewöhner et al., WO 9924433; eidem, US 6362178 (1999, 2002 both to Bayer AG). Effect on cGMP in human corpus cavernosum muscle cells: N. N. Kim et al., Life Sci. 69, 2249 (2001). Pharmacology: E. Bischoff et al., J. Urol. 165, 1316 (2001). Clinical trial in impotence: H. Porst et al., Int. J. Impotence Res. 13, 192 (2001); in erectile dysfunction: C. Stief et al., Int. J. Clin. Pract. 58, 230 (2004); F. Giuliano et al., BJU Int. 95, 110 (2005). Review of clinical experience in erectile dysfunction: S. Markou et al., Int. J. Impotence Res. 16, 470-478 (2004); M. Kendirci et al., Expert Opin. Pharmacother. 5, 923-932 (2004).

Sildenafil CAS Registry Number: 139755-83-2 西地那非

CAS Name: 1-[[3-(4,7-Dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo[4,3-d]pyrimidin-5-yl)-4-ethoxyphenyl]sulfonyl]-4-methylpiperazine
Additional Names: 5-[2-ethoxy-5-(4-methylpiperazinylsulfonyl)p...
Literature References: Orally active, selective type 5 cGMP phosphodiesterase inhibitor. Prepn: A. S. Bell et al., EP 463756; eidem, US 5250534 (1992, 1993 both to Pfizer). Structure-activity study: N. K. Terrett et al., Bioorg. Med. Chem. Lett. 6, 1819 (1996). Clinical trial in impotence: I. Goldstein et al., N. Engl. J. Med. 338, 1397 (1998). Review of pharmacology: M. Boolell et al., Int. J. Impot. Res. 8, 47-52 (1996); of clinical experience: D. G. Hatzichristou, ibid. 14, Suppl. 1, S43-S52 (2002). Clinical evaluation in pulmonary hypertension: B. K. S. Sastry et al., J. Am. Coll. Cardiol. 43, 1149 (2004).

Ampicillin CAS Registry Number: 69-53-4 氨苄西林

CAS Name: (2S,5R,6R)-6-[[(2R)-Aminophenylacetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: 6-[D(-)-a-aminophenylacetamido]penicillanic acid;...
Literature References: Orally active, semi-synthetic antibiotic; structurally related to penicillin. Prepn: Doyle et al., US 2985648 (1961); eidem, GB 902703 (1962 to Beecham); Doyle et al., J. Chem. Soc. 1962, 1440. Prepn of the trihydrate: D. A. Johnson, G. A. Hardcastle, US 3157640 (1964 to Bristol-Myers); of the anhydrous crystalline form: N. H. Grant, H. E. Alburn, US 3144445 (1964 to Am. Home Prods.). Alternate syntheses: Dane, Dockner, Ber. 98, 789 (1965); F. Kajfez et al., J. Heterocycl. Chem. 13, 561 (1976). LC determn: M. Margosis, J. Assoc. Off. Anal. Chem. 70, 206 (1987). Series of articles on pharmacology and antibacterial activity: Br. Med. J. 2, 193-206 (1961). Comprehensive description: E. Ivashkiv, Anal. Profiles Drug Subs. 2, 1-61 (1973). Review of pharmacology and clinical efficacy in combination with sulbactam, q.v.: D. M. Campoli-Richards, R. N. Brogden, Drugs 33, 577-609 (1987).

Glypinamide CAS Registry Number: 1228-19-9 格列平脲

CAS Name: 4-Chloro-N-[[(hexahydro-1H-azepin-1-yl)amino]carbonyl]benzenesulfonamide
Additional Names: 1-(p-chlorophenylsulfonyl)-3-(hexahydro-1H-azepin-1-yl)urea; azepinamide
Trademarks: Pari...
Literature References: Orally active, sulfonylurea hypoglycemic agent. Prepn: Wright, GB 887886 (1962 to Upjohn); Wright, Willette, J. Med. Pharm. Chem. 5, 815 (1962).

Aliskiren CAS Registry Number: 173334-57-1 阿利吉仑

CAS Name: (aS,gS,dS,zS)-d-Amino-N-(3-amino-2,2-dimethyl-3-oxopropyl)-g-hydroxy-4-methoxy-3-(3-methoxypropoxy)-a,z-bis(1-methylethyl)benzeneoctanamide
Additional Names: (2S,4S,5S,7S)-5-amino-N-(...
Literature References: Orally active, synthetic nonpeptide renin inhibitor. Prepn: R. Göschke et al., EP 678503; eidem, US 5559111 (1995, 1996 both to Ciba-Geigy); H, Rüeger et al., Tetrahedron Lett. 41, 10085 (2000). Synthesis: A. Dondoni et al., ibid. 42, 4819 (2001). Determn by HPLC in biological fluids: G. Lefevre, S. Gauron, J. Chromatogr. B 738, 129 (2000); by RIA in plasma: G. Lefevre et al., J. Immunoassay 21, 65 (2000). Structure activity study: J. M. Wood et al., Biochem. Biophys. Res. Commun. 308, 698 (2003). Clinical pharmacology: J. Nussberger et al., Hypertension 39, e1 (2002). Clinical study: A. H. Gradman et al., Circulation 111, 1012 (2005). Review of development and therpaeutic potential: K. Allikmets, Curr. Opin. Invest. Drugs 3, 1479-1482 (2002).

Cefixime CAS Registry Number: 79350-37-1 头孢克肟

CAS Name: (6R,7R)-7-[[(2Z)-(2-Amino-4-thiazolyl)[(carboxymethoxy)imino]acetyl]amino]-3-ethenyl-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid
Additional Names: 7-[2-(2-amino-4-thia...
Literature References: Orally active, third generation cephalosporin antibiotic. Prepn: T. Takaya et al., EP 30630; eidem, US 4409214 (1981, 1983 both to Fujisawa); H. Yamanaka et al., J. Antibiot. 38, 1738 (1985). Synthesis and activity of (E)-isomer: K. Kawabata et al., Chem. Pharm. Bull. 34, 3458 (1986). Mechanism of action: Y. Shigi et al., J. Antibiot. 37, 790 (1984). Comparative antibacterial spectrum in vitro and in vivo: T. Kamimura et al., Antimicrob. Agents Chemother. 25, 98 (1984). In vitro activity and b-lactamase stability: H. C. Neu et al., ibid. 26, 174 (1984). HPLC determn in human plasma and urine: Y. Tokuma et al., J. Chromatogr. 311, 339 (1984). Pharmacokinetics in humans: D. R. P. Guay et al., Antimicrob. Agents Chemother. 30, 485 (1986). Clinical trial in urinary tract infections: J. Levenstein et al., S. Afr. Med. J. 70, 455 (1986); A. Irvani et al., Am. J. Med. 85, Suppl. 3A, 17 (1988); in respiratory infections: R. Kiani et al., ibid. 6.

Dasatinib CAS Registry Number: 302962-49-8 达沙替尼

CAS Name: N-(2-Chloro-6-methylphenyl)-2-[[6-[4-(2-hydroxyethyl)-1-piperazinyl]-2-methyl-4-pyrimidinyl]amino]-5-thiazolecarboxamidePercent Composition: C 54.15%, H 5.37%, Cl 7.26%, N 20.09%, O 6.56...
Literature References: Orally bioactive, ATP-competitive dual inhibitor of Src and Abl kinases. Prepn: J. Das et al., WO 0062778; eidem US 6596746 (2000, 2003 both to Bristol-Myers Squibb); and Src/Abl kinase inhibition study: L. J. Lombardo et al., J. Med. Chem. 47, 6658 (2004). In vivo evaluation vs imatinib-resistant mutants in chronic myeloid leukemia: N. P. Shah et al., Science 305, 399 (2004). Mechanism of action study: M. R. Burgess et al., Proc. Natl. Acad. Sci. USA 102, 3395 (2005). Review of therapeutic potential in chronic myeloid leukemia: T. O'Hare et al., Curr. Opin. Genet. Dev. 16, 92-99 (2006).