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

Lopinavir CAS Registry Number: 192725-17-0 洛匹那韦

CAS Name: (aS)-N-[(1S,3S,4S)-4-[[(2,6-Dimethylphenoxy)acetyl]amino]-3-hydroxy-5-phenyl-1-(phenylmethyl)pentyl]tetrahydro-a-(1-methylethyl)-2-oxo-1(2H)-pyrimidineacetamide
Additional Names: (aS)...
Literature References: HIV protease inhibitor; analog of ritonavir, q.v. Prepn: H. L. Sham et al., WO 9721685; idem et al., US 5914332 (1997, 1999 both to Abbott); E. J. Stoner et al., Org. Process Res. Dev. 3, 145 (1999). Protease inhibition and pharmacokinetics: H. L. Sham et al., Antimicrob. Agents Chemother. 42, 3218 (1998). In vitro metabolism study: G. N. Kumar et al., Drug Metab. Dispos. 27, 86 (1999). Pharmacokinetic enhancement by ritonavir: G. N. Kumar et al., ibid. 902. Clinical trial with ritonavir in HIV infection: S. Walmsley et al., N. Engl. J. Med. 346, 2039 (2002).

Fosamprenavir CAS Registry Number: 226700-79-4 福沙那韦

CAS Name: [(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-1-(phenylmethyl)-2-(phosphonooxy)propyl]carbamic acid C-[(3S)-tetrahydro-3-furanyl] ester
Additional Names: (3S)-tetrahydro...
Literature References: HIV protease inhibitor; water soluble prodrug of amprenavir, q.v. Prepn: R. D. Tung et al., WO 9933815; eidem, US 6559137 (1999, 2003 both to Vertex). Prepn of crystalline calcium salt: I. G. Armitage et al., WO 0004033 (2000 to Glaxo); eidem, US 6514953 (2003 to SKB). Clinical pharmacokinetics: C. Falcoz et al., J. Clin. Pharmacol. 42, 887 (2002). Review of pharmacology and clinical experience in HIV: T. M. Chapman et al., Drugs 64, 2101-2124 (2004); C. Arvieux, O. Tribut, ibid. 65, 633-659 (2005).

Pitavastatin CAS Registry Number: 147511-69-1 匹伐他汀

CAS Name: (3R,5S,6E)-7-[2-Cyclopropyl-4-(4-fluorophenyl)-3-quinolinyl]-3,5-dihydroxy-6-heptenoic acid
Additional Names: itavastatin; nisvastatin
Percent Composition: C 71.24%, H 5.74%, F 4.5...
Literature References: HMG CoA reductase inhibitor. Prepn: Y. Fujikawa et al., EP 304063; eidem, US 5011930 (1989, 1991 both to Nissan Chem. Ind.). Prepn of lactone: S. Takano et al., Tetrahedron: Asymmetry 4, 201 (1993). Chiral synthesis: M. Suzuki et al., Bioorg. Med. Chem. Lett. 9, 2977 (1999). Structure-activity study: idem et al., Bioorg. Med. Chem. 9, 2727 (2001). Pharmacology: T. Aoki et al., Arzneim.-Forsch. 47, 904 (1997). HPLC determn in plasma: J. Kojima et al., J. Chromatogr. B 724, 173 (1999). Metabolism: I. Yamada et al., Xenobiotica 33, 789 (2003). Clinical comparison with pravastatin: Y. Saito et al., Atherosclerosis 162, 373 (2002). Clinical evaluation in hypercholesterolemia: S. Park et al., Clin. Ther. 27, 1074 (2005). Review of pharmacokinetics and clinical experience: K. Kajinami et al., Cardiovasc. Drug Rev. 21, 199-215 (2003); R. Y. A. Mukhtar et al., Int. J. Clin Pract. 59, 239-252 (2005).

Cerivastatin CAS Registry Number: 145599-86-6 西立伐他汀

CAS Name: (3R,5S,6E)-7-[4-(4-Fluorophenyl)-5-(methoxymethyl)-2,6-bis(1-methylethyl)-3-pyridinyl]-3,5-dihydroxy-6-heptenoic acid
Additional Names: (3R,5S,6E)-7-[4-(p-fluorophenyl)-2,6-diisopropy...
Literature References: HMG-CoA reductase inhibitor. Prepd and claimed as methyl ester: R. Angerbauer et al., EP 325130; eidem, US 5006530; as (+)-form sodium salt: eidem, US 5177080 (1989, 1991, 1993 all to Bayer). Determn in plasma by fluorescence linked LC: G. J. Krol et al., J. Pharm. Biomed. Anal. 11, 1269 (1993); by HPLC: eidem, Methodol. Surv. Bioanal. Drugs 23, 147 (1994). Effects on LDL receptor levels: G. C. Ness et al., Arch. Biochem. Biophys. 325, 242 (1996). Pharmacokinetics in dogs and rats: W. Steinke et al., Jpn. Pharmacol. Ther. 24 Suppl. 9, S1217 (1996). Clinical trial in hyperlipidemia: N. Nakaya et al., ibid. S1381.

Atorvastatin CAS Registry Number: 134523-00-5 阿伐他汀

CAS Name: (bR,dR)-2-(4-Fluorophenyl)-b,d-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid
Percent Composition: C 70.95%, H 6.31%, F 3.40%, N 5.01%, O 1...
Literature References: HMG-CoA reductase inhibitor. Prepn: B. D. Roth, EP 409281; idem, US 5273995 (1991, 1993 both to Warner-Lambert); K. L. Baumann et al., Tetrahedron Lett. 33, 2283 (1992). Solubility and kinetic studies: A. S. Kearney et al., Pharm. Res. 10, 1461 (1993). LC/MS/MS determn in serum: M. Jemal et al., Rapid Commun. Mass Spectrom. 13, 1003 (1999). Clinical pharmacokinetics: D. D. Cilla, Jr. et al., Clin. Pharmacol. Ther. 60, 687 (1996). Review of pharmacology and clinical experience: H. S. Yee, N. T. Fong, Ann. Pharmacother. 32, 1030-1043 (1998); of efficacy in diabetic patients: K. F. Croom, G. L. Plosker, Drugs 65, 137-152 (2005).

Rosuvastatin CAS Registry Number: 287714-41-4 罗伐他汀

CAS Name: (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-(1-methylethyl)-2-[methyl(methylsulfonyl)amino]-5-pyrimidinyl]-3,5-dihydroxy-6-heptenoic acid
Percent Composition: C 54.87%, H 5.86%, F 3.95%, N 8.7...
Literature References: HMG-CoA reductase inhibitor. Prepn: K. Hirai et al., EP 521471; eidem, US 5260440 (both 1993 to Shionogi); M. Watanabe et al., Bioorg. Med. Chem. 5, 437 (1997). Pharmacology: F. McTaggart et al., Am. J. Cardiol. 87, Suppl., 28B (2001). Comparative clinical trial with atorvastatin: M. Davidson et al., ibid. 89, 268 (2002); in metabolic syndrome: A. F. H. Stalenhoef et al., Eur. Heart J. 26, 2664 (2005); in African-American patients: K. C. Ferdinand et al., Am. J. Cardiol. 97, 229 (2006). Pharmacokinetics and pharmacogenetics in Asian and white ethnic groups: E. Lee et al., Clin. Pharmacol. Ther. 78, 330 (2005). Review of therapeutic potential: K. C. Ferdinand, Expert Opin. Pharmacother. 6, 1897-1910 (2005).

Pravastatin Sodium CAS Registry Number: 81131-70-6 普伐他汀钠

CAS Name: (bR,dR,1S,2S,6S,8S,8aR)-1,2,6,7,8,8a-Hexahydro-b,d,6-trihydroxy-2-methyl-8-[(2S)-2-methyl-1-oxobutoxy]-1-naphthaleneheptanoic acid monosodium salt
Additional Names: sodium (+)-(3R,5R)...
Literature References: HMG-CoA reductase inhibitor; bioactive metabolite of mevastatin, q.v. Prepn by microbial hydroxylation: A. Terahara, M. Tanaka, DE 3122499; eidem, US 4346227 (1981, 1982 both to Sankyo); N. Serizawa et al., J. Antibiot. 36, 604 (1983). Structure elucidation: H. Haruyama et al., Chem. Pharm. Bull. 34, 1459 (1986). HPLC determn in biological fluids: S. Bauer et al., J. Chromatogr. B 818, 257 (2005). Effect on serum lipid concentration: N. Nakaya et al., Atherosclerosis 61, 125 (1986); on hepatic metabolism of cholesterol: E. Reihnér et al., N. Engl. J. Med. 323, 224 (1990). Clinical comparison with probucol, q.v.: G. Yoshino et al., Lancet 2, 740 (1986). Clinical reduction of risk of major cardiovascular events in patients with coronary heart disease: LIPID Study Group, N. Engl. J. Med. 339, 1349 (1998). Clinical effect on risk of stroke: H. D. White et al., ibid. 343, 317 (2000).

Simvastatin CAS Registry Number: 79902-63-9 辛伐他汀,斯伐他汀

CAS Name: 2,2-Dimethylbutanoic acid (1S,3R,7S,8S,8aR)-1,2,3,7,8,8a-hexahydro-3,7-dimethyl-8-[2-[(2R,4R)-tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl]ethyl]-1-naphthalenyl ester
Additional Names: 2,...
Literature References: HMG-CoA reductase inhibitor; synthetic analog of lovastatin, q.v. Prepn: A. K. Willard et al., EP 33538; W. F. Hoffman et al., US 4444784 (1981, 1984 both to Merck Co.); W. F. Hoffman et al., J. Med. Chem. 29, 849 (1986). Comprehensive description: D. K. Ellison et al., Anal. Profiles Drug Subs. Excip. 22, 359-388 (1993). Effect on survival in CHD: Scandinavian Simvastatin Survival Study Group, Lancet 344, 1383 (1994). Clinical trial in primary hypercholesterolemia: L. Ose et al., Clin. Cardiol. 23, 39 (2000); in mixed hyperlipidemia: E. Stein et al., Am. J. Cardiol. 86, 406 (2000).

Erdosteine CAS Registry Number: 84611-23-4 厄多司坦

CAS Name: [[2-Oxo-2-[(tetrahydro-2-oxo-3-thienyl)amino]ethyl]thio]acetic acid
Additional Names: (±)-[[[(tetrahydro-2-oxo-3-thienyl)carbamoyl]methyl]thio]acetic acid; DL-S-[2-[N-3-(2-oxotet...
Literature References: Homocysteine thiolactone derivative with mucomodulating activity. Prepn: J. Gonella, EP 61386; idem, US 4411909 (1982, 1983 both to Refarmed); M. Gobetti et al., Farmaco Ed. Sci. 41, 69 (1986). Clinical trial in bronchitis: G. Ricevuti et al., Thorax 43, 585 (1988). Clinical effect on a1-antitrypsin levels in cigarette smokers: M. Vagliasindi, G. B. Fregnan, Int. J. Clin. Pharmacol. Ther. Toxicol. 27, 238 (1989).

BIGCHAP CAS Registry Number: 86303-22-2 (3a,5b,7a,12a)-N,N-双[3-(D-葡萄糖酰氨基)丙基]-3,7,12-三羟基胆甾烷-24-胺

CAS Name: (3a,5b,7a,12a)-N,N-Bis[3-(D-gluconoylamino)propyl]-3,7,12-trihydroxycholan-24-amide
Percent Composition: C 57.45%, H 8.61%, N 4.79%, O 29.15%
Literature References: Homogeneous nonionic detergent; derivative of cholic acid, q.v. Prepn: L. M. Hjelmeland et al., Anal. Biochem. 130, 485 (1983). QSAR study as surfactant: P. Campbell et al., Biotechnol. Bioeng. 64, 527 (1999). Use in protein purification via hydrophobic interaction displacement chromatography: K. M. Sunasara et al., ibid. 82, 330 (2003). Clinical evaluation as a transduction enhancing agent in gene therapy: J. Kuball et al., J. Clin. Oncol. 20, 957 (2002).