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

Octyl Salicylate CAS Registry Number: 118-60-5 水杨酸异辛酯

CAS Name: 2-Hydroxybenzoic acid 2-ethylhexyl ester
Additional Names: 2-ethylhexyl salicylate; octisalate
Trademarks: Eusolex OS (Merck KGaA); Neo Heliopan OS (Symrise)
Percent Composition...
Literature References: UV-B filter in sunscreens and cosmetics. Prepn: F. H. McMillan, J. A. King, J. Am. Chem. Soc. 67, 2271 (1945). In vitro skin penetration studies: K. A. Walters et al., Food Chem. Toxicol. 35, 1219 (1997); R. Jiang et al., J. Pharm. Sci. 86, 791 (1997). Determn in sun protection lotions by GC-MS: K. W. Ro et al., J. Chromatogr. A 688, 375 (1994); by HPTLC: E. Westgate, J. Sherma, Am. Lab. 32, 13 (2000).

Ensulizole CAS Registry Number: 27503-81-7 紫外线吸收剂UV-T

CAS Name: 2-Phenyl-1H-benzimidazole-5-sulfonic acid
Additional Names: phenylbenzimidazole sulfonic acid
Trademarks: Eusolex 232 (Merck KGaA); Neo Heliopan Hydro (Symrise); Parsol HS (DSM) Literature References: UV-B filter in sunscreens and cosmetics. Synergistic increase in SPF occurs in combination with oil-soluble UV absorbers. Prepn: V. G. Sayapin et al., Khim. Geterotsikl. Soedin. 5, 681 (1970), C.A. 73, 45409p (1970). See also: U. Heywang et al., US 5473079 (1995 to Merck Patent GmbH). DNA photosensitization study: C. Stevenson, R. J. H. Davies, Chem. Res. Toxicol. 12, 38 (1999). Photochemical studies: J. J. Inbaraj et al., Photochem. Photobiol. 75, 107 (2002). Fluorometric determn in urine: M. T. Vidal et al., Talanta 59, 591 (2003). Complexation with cyclodextrins: S. Scalia et al., Eur. J. Pharm. Sci. 22, 241 (2004).

Valganciclovir CAS Registry Number: 175865-60-8 缬更昔洛韦

CAS Name: L-Valine 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropyl ester
Additional Names: 2-[(2-amino-1,6-dihydro-6-oxo-9H-purin-9-yl)methoxy]-3-hydroxypropanyl-L-valinate...
Literature References: Valine ester prodrug of ganciclovir, q.v. Prepn: J. J. Nestor et al., EP 694547; eidem, US 6083953 (1996, 2000 both to Hoffmann-La Roche). HPLC determn in plasma: R. Chan et al., J. Pharm. Biomed. Anal. 21, 647 (1999). Clinical pharmacokinetics in HIV- and CMV-positive patients: F. Brown et al., Clin. Pharmacokinet. 37, 167 (1999); in liver transplant patients: M. D. Pescovitz et al., Antimicrob. Agents Chemother. 44, 2811 (2000). Clinical trial in cytomegalovirus retinitis: D. F. Martin et al., N. Engl. J. Med. 346, 1119 (2002).

Magnesium Borate CAS Registry Number: 13703-82-7 偏硼酸镁

Additional Names: Antifungin
Percent Composition: B 19.67%, Mg 22.11%, O 58.22%
Literature References: Various magnesium borate minerals occur in nature. These include: ascharite, camsellite, inderite, kotoite, kurnakovite, paternoite, pinnoite, szaibelyite.

Vatalanib CAS Registry Number: 212141-54-3 伐拉尼布

CAS Name: N-(4-Chlorophenyl)-4-(4-pyridinylmethyl)-1-phthalazinamine
Additional Names: 1-(4-chloroanilino)-4-(4-pyridylmethyl)phthalazinePercent Composition: C 69.26%, H 4.36%, Cl 10.22%, N 16....
Literature References: Vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitor; vascular endothelial angiogenesis inhibitor. Prepn: G. Bold et al., WO 9835958; eidem, US 6258812 (1998, 2001 both to Novartis); eidem, J. Med. Chem. 43, 2310 (2000). Enzyme inhibition study and pharmacology: J. M. Wood et al., Cancer Res. 60, 2178 (2000). Antiangiogenic activity: J. Drevs et al., ibid. 62, 4015 (2002). Clinical pharmacokinetics: B. Morgan et al., J. Clin. Oncol. 21, 3955 (2003). Review of mechanism of action: P. Furet, P. W. Manley ACS Symp. Ser. 796, 282-298 (2001); and therapeutic potential: A. L. Thomas et al., Semin. Oncol. 30, Suppl. 6, 32-38 (2003).

Serotonin CAS Registry Number: 50-67-9 5-羟基色胺

CAS Name: 3-(2-Aminoethyl)-1H-indol-5-ol
Additional Names: 5-hydroxytryptamine; 3-(b-aminoethyl)-5-hydroxyindole; 5-hydroxy-3-(b-aminoethyl)indole; enteramine; thrombocytin; thrombotonin; 5-HT<...
Literature References: Vasoactive amine found in tissues and fluids of vertebrates and invertebrates. Extraction of enteramine from rabbit tissue, pharmacology: V. Erspamer, Arch. Exp. Pathol. Pharmakol. 196, 343 (1940). Isoln of 5-HT from beef serum: M. M. Rapport et al., Science 108, 329 (1948); eidem, J. Biol. Chem. 176, 1237, 1243 (1948); M. M. Rapport, ibid. 180, 961 (1949). Identity with enteramine, the enterochromaffin cell hormone: V. Erspamer, B. Asero, Nature 169, 800 (1952). Ultrastructural localization in enterochromaffin cells: R. D. Dey, J. Hoffpauir, J. Histochem. Cytochem. 32, 661 (1984). Synthesis starting with 5-benzyloxyindole: M. E. Speeter et al., J. Am. Chem. Soc. 73, 5514 (1951); K. E. Hamlin, US 2715129 (1955 to Abbott). Alternate routes: R. Justoni, R. Pessina, US 2947757 (1960 to Vismara). Pharmacology: G. Reid, M. Rand, Nature 169, 801 (1952). Existence of multiple serotonin receptors: S. J. Peroutka, S. H. Snyder, Mol. Pharmacol. 16, 687 (1979); G. Engel et al., Arch. Pharmacol. 324, 116 (1983); W. Feniuk et al., Eur. J. Pharmacol. 96, 71 (1983). Extraneural synthesis in CNS: C. Maruki et al., J. Neurochem. 43, 316 (1984). Effect on smooth muscle: W. Feniuk et al., loc. cit. Activity as neurotransmitter: S. G. Griffith et al., Brain Res. 247, 388 (1982). Role in hemostasis: F. De Clerck et al., Agents Actions 15, 627 (1984). Series of articles on role in hypertension, Raynaud's phenomenon and platelet activation: J. Cardiovasc. Pharmacol. 7, Suppl. 7, 1-182 (1985). Review of role in migraine: E. T. MacKenzie et al., Cephalalgia 5, 69-78 (1985). Review: V. Erspamer in E. Jucker, Prog. Drug Res. 3, 151-367 (1961). Books: Serotonin in Health and Disease vols. I-V, W. B. Essman, Ed. (Spectrum, New York, 1978); Adv. Exp. Med. 133, entitled "Serotonin: Current Aspects of Neurochemistry and Function," B. Haber, Ed. (1981) 824 pp; Serotonin and the Cardiovascular System, P. M. Vanhoutte, Ed. (Raven Press, New York, 1985) 280 pp. See also Bufotenine and Ketanserin.

Droprenilamine CAS Registry Number: 57653-27-7 氢普拉明

CAS Name: N-(2-Cyclohexyl-1-methylethyl)-g-phenylbenzenepropanamine
Additional Names: (±)-N-(3,3-diphenylpropyl)-a-methylcyclohexaneethylamine; droprenylamine
Percent Composition: C 85....
Literature References: Vasodilator with antiarrhythmic and hypotensive activity. Prepn: M. Carissimi et al., DE 2521113 (1976 to Maggioni), C.A. 84, 164388t (1976). Synthesis and pharmacological study: G. Carenini et al., Arzneim.-Forsch. 26, 2127 (1976). Hemodynamic and metabolic effects: R. J. Marshall, J. R. Parratt, Br. J. Pharmacol. 59, 311 (1977). Clinical evaluation: F. Rengo et al., G. Ital. Cardiol. 10, 473 (1980).

Dihydralazine CAS Registry Number: 484-23-1 双肼屈嗪

CAS Name: 2,3-Dihydro-1,4-phthalazinedione dihydrazone
Additional Names: 1,4-dihydrazinophthalazine
Percent Composition: C 50.52%, H 5.30%, N 44.18%
Literature References: Vasodilator. Prepn: J. Druey, US 2484785 (1949 to Ciba); J. Druey, B. H. Ringier, Helv. Chim. Acta 34, 195 (1951); Zerweck, Kunze, US 2786839 (1957 to Cassella Farbw.). Pharmacology: P. A. Van Zwieten, Arzneim.-Forsch. 18, 79 (1968). Mechanism of action: I. W. Reimann et al., Clin. Sci. 61, 319s (1981); eidem, Clin. Exp. Pharmacol. Physiol. 12, 79 (1985). Cerebrovascular effects in rats: L. M. Auer et al., Acta Med. Scand. Suppl. 678, 73 (1983); D. I. Barry et al., Stroke 15, 102 (1984). Hemodynamic responses in man: G. G. Belz, Clin. Pharmacol. Ther. 37, 48 (1985). Clinical studies: A. Salvadeo et al., Int. J. Clin. Pharmacol. Ther. Toxicol. 19, 372 (1981); P. I. Salmela et al., Ann. Clin. Res. 13, 433 (1981). Toxicity data: G. Steiner et al., J. Med. Chem. 24, 59 (1981).

Fasidotril CAS Registry Number: 135038-57-2 法西多曲

CAS Name: N-[(2S)-3-(Acetylthio)-2-(1,3-benzodioxol-5-ylmethyl)-1-oxopropyl]-L-alanine phenylmethyl ester
Additional Names: N-[(S)-a-(mercaptomethyl)-3,4-(methylenedioxy)-hydrocinnamoyl]-L-alan...
Literature References: Vasopeptidase inhibitor (VPI) exhibiting characteristic dual metalloprotease inhibition of neutral endopeptidase (NEP) and angiotensin converting enzyme (ACE). Prepn: J.-C. Plaquevent et al., EP 419327; eidem, US 5670531 (1991, 1997 both to Soc. Civile Bioprojet). Absolute configuration: V. Grosset et al., Tetrahedron: Asymmetry 14, 2335 (2003). Enzyme inhibition activity: C. Gros et al., Proc. Natl. Acad. Sci. USA 88, 4210 (1991). Preclinical and clinical pharmacology: S. Laurent et al., Hypertension 35, 1148 (2000). Review of design and pharmacology: J. Bralet et al., Cardiovasc. Drug Rev. 18, 1-24 (2000); of therapeutic potential: F. Ozdener, V. Ozdemir, Curr. Opin. Invest. Drugs 4, 1113-1119 (2003).

Cyanuric Chloride CAS Registry Number: 108-77-0 氰尿酰氯

CAS Name: 2,4,6-Trichloro-1,3,5-triazine
Additional Names: trichloro-s-triazine
Percent Composition: C 19.54%, Cl 57.68%, N 22.79%
Literature References: Versatile coupling agent for proteins and nucleic acids; reagent in synthetic organic chemistry. Prepn: A. Gautier, Ann. 141, 122 (1867); H. Herlinger, Angew. Chem. 76, 437 (1964). Structural studies: A. W. Hofmann, Ber. 19, 2061 (1886); R. A. Pascal, Jr., D. M. Ho, Tetrahedron Lett. 33, 4707 (1992); S. J. Maginn et al., ibid. 34, 4349 (1993); V. Krishnakumar, R. Ramasamy, Spectrochim. Acta A 61, 3112 (2005). Polarographic determn in air: V. Stará et al., Anal. Chim. Acta 147, 371 (1983). Synthetic applications as a chlorinating reagent for alcohols: S. R. Sandler et al., J. Org. Chem. 35, 3967 (1970); for carboxylic acids: K. Venkataraman, D. R. Wagle, Tetrahedron Lett. 20, 3037 (1979); in macrocyclic lactonization: eidem, ibid. 21, 1893 (1980); as a Beckmann rearrangement catalyst: Y. Furuya et al., J. Am. Chem. Soc. 127, 11240 (2005); as a dehydrating agent: K. P. Haval et al., Tetrahedron 62, 937 (2006). Use as a linking agent in molecular biology applications: H.-D. Hunger et al., Anal. Biochem. 156, 286 (1986); idem et al., ibid. 165, 45 (1987); R. A. Abuknesha et al., J. Immunol. Methods 306, 211 (2005).