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

Delapril CAS Registry Number: 83435-66-9 地拉普利

CAS Name: N-[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl-N-(2,3-dihydro-1H-inden-2-yl)glycine
Additional Names: N-[N-[(S)-1-(ethoxycarbonyl)-3-phenylpropyl]-L-alanyl]-N-(indan-2-yl)glycine...
Literature References: Angiotensin-converting enzyme (ACE) inhibitor. Prepn: Y. Oka et al., EP 51391; eidem, US 4385051 (1982, 1983 both to Takeda); J. T. Suh et al., Eur. J. Med. Chem. - Chim. Ther. 20, 563 (1985); A. Miyake et al., Chem. Pharm. Bull. 34, 2852 (1986). Pharmacology in animals: Y. Inada et al., Jpn. J. Pharmacol. 42, 1 (1986); eidem, ibid., 99. Pharmacology and metabolism in humans: T. Ogihara et al., Curr. Ther. Res. 41, 809 (1987). Pharmacokinetics and evaluation in hypertension: H. Shionoiri et al., Clin. Pharmacol. Ther. 41, 74 (1987).

Enalapril CAS Registry Number: 75847-73-3 依那普利

CAS Name: N-[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]-L-alanyl-L-proline
Additional Names: 1-[N-[(S)-1-carboxy-3-phenylpropyl]-L-alanyl]-L-proline 1'-ethyl ester
Percent Composition: C 63.81%...
Literature References: Angiotensin-converting enzyme (ACE) inhibitor; de-esterified in vivo to its active diacid metabolite, enalaprilat, q.v. Prepn: A. A. Patchett et al., Nature 288, 280 (1980); eidem, EP 12401; E. E. Harris et al., US 4374829 (1980, 1983 both to Merck Co.). Pharmacology: D. M. Gross et al., J. Pharmacol. Exp. Ther. 216, 552 (1981); C. S. Sweet et al., ibid. 558. Bioavailability and metabolism: E. H. Ulm, Drug Metab. Rev. 14, 99 (1983). Comprehensive description: D. P. Ip, G. S. Brenner, Anal. Profiles Drug Subs. 16, 207-243 (1987). Clinical trial in congestive heart failure: Consensus Trial Study Group, N. Engl. J. Med. 316, 1429 (1987). Review of clinical experience in hypertension: H. J. Gomez et al., J. Cardiovasc. Pharmacol. 15, Suppl. 3, S26-S29 (1990); of clinical pharmacokinetics: R. J. MacFadyen et al., Clin. Pharmacokinet. 25, 274-282 (1993); of combination with hydrochlorothiazide: P. L. Malini, Adv. Ther. 10, 253-262 (1993).

Zofenopril CAS Registry Number: 81872-10-8 佐芬普利

CAS Name: (4S)-1-[(2S)-3-(Benzoylthio)-2-methyl-1-oxopropyl]-4-(phenylthio)-L-proline
Additional Names: [1(S),4(S)]-1-(3-mercapto-2-methyl-1-oxopropyl)-4-phenyl-thio-L-proline-S-benzoylester Literature References: Angiotensin-converting enzyme (ACE) inhibitor; de-esterified in vivo to its active sulfhydryl-containing metabolite, zofenoprilat. Prepn: M. A. Ondetti, J. Krapcho, GB 2028327; eidem, US 4316906 (1980, 1982 both to E. R. Squibb Sons). LC/MS/MS determn in plasma: L. Dal Bo et al., J. Chromatogr. B 749, 287 (2000). Role of sulfhydryl group in improvement of endothelial dysfunction: H. Buikema et al., Br. J. Pharmacol. 130, 1999 (2000); L. Cominacini et al., Am. J. Hypertens. 15, 891 (2002). Clinical comparison with lisinopril of effect on post-infarction survival: C. Borghi, E. Ambrosioni, Am. Heart J. 145, 80 (2003). Review of properties and pharmacokinetics: A. Subissi et al., Cardiovasc. Drug Rev. 17, 115-133 (1999); of clinical efficacy in cardiovascular diseases: C. Borghi et al., Expert Opin. Pharmacother. 5, 1965-1977 (2004).

Cilazapril CAS Registry Number: 88768-40-5 西拉普利

CAS Name: (1S,9S)-9-[[(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl]amino]octahydro-10-oxo-6H-pyridazino[1,2-a][1,2]diazepine-1-carboxylic acid
Additional Names: (1S,9S)-9-[[(S)-1-carboxy-3-phenylprop...
Literature References: Angiotensin-converting enzyme (ACE) inhibitor; hydrolyzed in vivo to the active diacid metabolite. Prepn: M. R. Attwood et al., DE 3317290; eidem, US 4512924 (1983, 1985 both to Hoffmann-La Roche); eidem, J. Chem. Soc. Perkin Trans. 1 1986, 1011. HPLC determn in urine and pharmaceutical formulations: J. A. Prieto et al., J. Chromatogr. B 714, 285 (1998). Pharmacology: I. L. Natoff et al., J. Cardiovasc. Pharmacol. 7, 569 (1985). Review of clinical pharmacology: C. H. Kleinbloesem et al., Am. J. Med. 87, Suppl. 6B, 45S-49S (1989). Review of clinical experience in hypertension: T. Szucs, Drugs 41, Suppl. 1, 18-24 (1991); in chronic heart failure: L. Dössegger et al., J. Cardiovasc. Pharmacol. 24, Suppl. 3, S38-S41 (1994); in combination with hydrochlorothiazide: R. C. Pordy, Cardiology 86, 41-48 (1995).

Moveltipril CAS Registry Number: 85856-54-8 莫维普利

CAS Name: N-(Cyclohexylcarbonyl)-D-alanyl-(2S)-3-mercapto-2-methylpropanoyl-L-proline
Additional Names: N-[3-(N-cyclohexanecarbonyl-D-alanylthio)-2-methylpropanoyl]-L-proline; (-)-N-[(S)-[3-(N-...
Literature References: Angiotensin-converting enzyme (ACE) inhibitor; structural analog of captopril. Prepn: S. Tanaka et al., BE 893553 (1982 to Chugai), C.A. 98, 215995n (1983). Pharmacology: K. Sakai et al., Tohoku J. Exp. Med. 152, 363 (1987). Hemodynamic effects in dogs: K. Noguchi et al., Jpn. J. Pharmacol. 40, 373 (1986). Antihypertensive activity: J. Aono et al., Arch. Int. Pharmacodyn. 292, 203 (1988). Tissue specific ACE inhibitory activity: K. Sakai et al., ibid. 294, 228 (1988). Determn by radioimmunoassay: Y. Hinohara et al., J. Pharmacobio-Dyn. 11, 411 (1988).

Avoparcin CAS Registry Number: 37332-99-3 阿伏帕星

Trademarks: Avotan (Roche)
Literature References: Animal feed glycopeptide antibiotic complex produced by Streptomyces candidus. Prodn: M. P. Kunstmann, J. N. Porter, US 3338786 (1967 to Am. Cyanamid). Fermentation, isoln, characterization: M. P. Kunstmann et al., Antimicrob. Agents Chemother. 8, 242 (1968). Isoln, purif of major components: W. J. McGahren et al., J. Antibiot. 36, 1671 (1983). HPLC separation of a-, b-avoparcin: F. Sztaricskai et al., ibid. 1691. Structural studies: J. J. Hlavka et al., Tetrahedron Lett. 1974, 175; W. J. McGahren et al., J. Am. Chem. Soc. 101, 2237 (1979). Structure: eidem, ibid. 102, 1671 (1980). Stereochemistry and epimerization: G. A. Ellestad et al., J. Antibiot. 36, 1683 (1983). Relationship between structure, antibacterial activity: S.W. Fesik et al., Mol. Pharmacol. 25, 275 (1984). Effect on resistance patterns in chickens: J. R. Walton, Zentralbl. Veterinaermed. (B) 25, 290 (1978), C.A. 89, 173507 (1978). Prevention of exptly induced necrotic enteritis in chickens: J. F. Prescott, Avian Dis. 23, 1072 (1979). Effect on feedlot performance: R. J. Johnson et al., J. Anim. Sci. 48, 1338 (1979).

Zeranol CAS Registry Number: 26538-44-3 α玉米赤霉醇

CAS Name: (3S,7R)-3,4,5,6,7,8,9,10,11,12-Decahydro-7,14,16-trihydroxy-3-methyl-1H-2-benzoxacyclotetradecin-1-one
Additional Names: 6-(6,10-dihydroxyundecyl)-b-resorcylic acid m-lactone; a-zeara...
Literature References: Animal growth promotant prepd from zearalenone, q.v.: E. B. Hodge et al., US 3239345 (1966 to Commercial Solvents). Stereoselective prepn and abs config: G. Snatzke et al., Helv. Chim. Acta 69, 734 (1986). TLC determn in plasma and tissues: M. B. Medina, N. Nagdy, J. Chromatogr. 614, 315 (1993). Growth regulating and repartitioning effects in cattle: P. G. Lemieux et al., J. Anim. Sci. 68, 1702 (1990). Review: R. S. Baldwin et al., Regul. Toxicol. Pharmacol. 3, 9-25 (1983).

Polidexide CAS Registry Number: 9064-92-0

CAS Name: Sephadex 2-(diethylamino)ethyl ether
Additional Names: dextran 2-(diethylamino)ethyl 2-[[2-(diethylamino)ethyl]diethylammonio]ethyl ether chloride hydrochloride epichlorohydrin crossl...
Literature References: Anion exchange resin containing quaternary ammonium groups. Bile acid sequestrant that has been used to reduce serum cholesterol. Prepn: GB 1013585 (1965 to Pharmacia AB). Clinical evaluation in hyperlipidemia: R. J. C. Evans et al., Angiology 24, 22 (1973); S. Ritland et al., Scand. J. Gastroenterol. 10, 791 (1975). Review of use in chromatographic purification of proteins: D. M. Bollag, Methods Mol. Biol. 36, 11-22 (1994).

Sodium Lauryl Sulfate CAS Registry Number: 151-21-3 十二烷基硫酸钠

CAS Name: Sulfuric acid monododecyl ester sodium salt
Additional Names: sodium dodecyl sulfate; SDS
Trademarks: Irium
Percent Composition: C 49.98%, H 8.74%, Na 7.97%, O 22.19%, S 11.12%
Literature References: Anionic detergent prepd by sulfation of lauryl alcohol, followed by neutralization with sodium carbonate: A. Lottermoser, F. Stoll, Kolloid-Z. 63, 50 (1933). Surfactant properties: J. Powney, C. C. Addison, Trans. Faraday Soc. 33, 1244 (1937); E. E. Dreger et al., Ind. Eng. Chem. 36, 610 (1944). Use in electrophoretic sepn and mol wt estimation of proteins: A. L. Shapiro et al., Biochem. Biophys. Res. Commun. 28, 815 (1967); K. Weber, M. Osborn, J. Biol. Chem. 244, 4406 (1969); of glycopolypeptides: B. S. Leach et al., Biochemistry 19, 5734 (1980). Toxicity study: A. I. T. Walker et al., Food Cosmet. Toxicol. 5, 763 (1967). Review of toxicology: Ch. Gloxhuber, Arch. Toxicol. 32, 245-270 (1974).

Licostinel CAS Registry Number: 153504-81-5 6,7-二氯-5-硝基喹喔啉-2,3(1H,4H)-二酮

CAS Name: 6,7-Dichloro-1,4-dihydro-5-nitro-2,3-quinoxalinedione
Additional Names: 6,7-dichloro-5-nitro-1,4-dihydroquinoxaline-2,3-dionePercent Composition: C 34.81%, H 1.10%, Cl 25.69%, N 15.22...
Literature References: Antagonist of the NMDA receptor at the glycine site. Prepn: E. Weber, J. F. W. Keana, WO 9400124 (1994); eidem, US 5622952 (1997 to Univ. Oreg; Regents Univ. Calif.); J. F. W. Keana et al., J. Med. Chem. 38, 4367 (1995). Pharmacology in vitro: R. M. Woodward et al., Mol. Pharmacol. 47, 568 (1995); in vivo: B. D. Kretschmer et al., Eur. J. Pharmacol. 331, 109 (1997). Clinical evaluation and pharmacokinetics in acute stroke: G. W. Albers et al., Stroke 30, 508 (1999).