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

Gratioside CAS Registry Number: 53762-90-6

Percent Composition: C 63.30%, H 8.60%, O 28.11%
Literature References: Triterpene glycoside monohydrate from tubers of Gratiola officinalis L., Scrophulariaceae: Retzlaff, Arch. Pharm. 240, 561 (1902); Tschesche et al., Ann. 674, 196 (1964). Dec on hydrolysis into 1 mol gratiogenin and 2 mol glucose: Tschesche, Heesch, Ber. 85, 1067 (1952).

Tropesin CAS Registry Number: 65189-78-8

CAS Name: 1-(4-Chlorobenzoyl)-5-methoxy-2-methyl-1H-indole-3-acetic acid 2-carboxy-2-phenylethyl ester
Additional Names: d,l-2-phenyl-3-[1-(4-chlorobenzoyl)-5-methoxy-2-methylindole-3-acetoxy]p...
Literature References: Tropic acid ester of indomethacin, q.v. Prepn: L. Fisnerova et al., DE 2727629; eidem, US 4136194 (1978, 1979 both to Spofa). Clinical pharmacokinetics: I. Janku et al., Drugs Exp. Clin. Res. IX, 407 (1983). Review of pharmacology and clinical experience: J. Grimová et al., Drugs Today 27, 391-400 (1991).

Trospium Chloride CAS Registry Number: 10405-02-4 曲司氯胺

CAS Name: (1a,3b,5a)-3-[(Hydroxydiphenylacetyl)oxy]spiro[8-azoniabicyclo[3.2.1]octane-8,1'-pyrrolidinium] chloride
Additional Names: 3a-hydroxyspiro[1aH,5aH-nortropane-8,1'-pyrrolidinium] chlor...
Literature References: Tropine derivative with anticholinergic activity. Prepn: NL 6402155; R. Pfleger et al., US 3480626 (1964, 1969 both to Pfleger); H. Bertholdt et al., Arzneim.-Forsch. 17, 719 (1967). Pharmacology and toxicology in animals: H. Antweiler et al., ibid. 16, 1581 (1966). Inhibition of gastric motility and acid secretion in humans: G. Lux, P. Frühmorgen, Fortschr. Med. 96, 2113 (1978). Fluorimetric determn in plasma and urine: G. Schladitz-Keil et al., J. Chromatogr. 345, 99 (1985). Bioavailability: eidem, Arzneim.-Forsch. 36, 984 (1986). Clinical trial in bladder hyper-reflexia: H. Madersbacher et al., Br. J. Urol. 75, 452 (1995). Review in overactive bladder: N. R. Zinner, Expert Opin. Pharmacother. 6, 1409-1420 (2005).

Zinquin CAS Registry Number: 151606-29-0

CAS Name: [[2-Methyl-8-[[(4-methylphenyl)sulfonyl]amino]-6-quinolinyl]oxy]acetic acid
Additional Names: Zinquin A
Percent Composition: C 59.06%, H 4.70%, N 7.25%, O 20.70%, S 8.30%
Literature References: TSQ, q.v., derived membrane permeant fluorescent probe selective for Zn2+ in the presence of Ca2+ and Mg2+. Synthesis: I. B. Mahadevan et al., Aust. J. Chem. 49, 561 (1996). Coordination chemistry: C. J. Fahrni, T. V. O'Halloran, J. Am. Chem. Soc. 121, 11448 (1999); potentiometric coordination of fluorophore: K. M. Hendrickson et al., ibid. 125, 3889 (2003). Visualization of intracellular Zn2+ pools in pancreatic islets: P. D. Zalewski et al., J. Histochem. Cytochem. 42, 877 (1994); in apoptosis: P. J. Smith et al., Am. J. Physiol. Cell Physiol. 283, C609 (2002); G. R. Sauer et al., J. Cell Biochem. 88, 954 (2003).

Verazide CAS Registry Number: 93-47-0 维拉烟肼

CAS Name: 4-Pyridinecarboxylic acid [(3,4-dimethoxyphenyl)methylene]hydrazide
Additional Names: isonicotinic acid veratrylidenehydrazide; 1-isonicotinoyl-2-veratrylidenehydrazine; 3,4-dimethoxy...
Literature References: Tuberculostatic agent related to isoniazid. Prepd from isonicotinylhydrazine and veratraldehyde: Fox, Gibas, J. Org. Chem. 18, 983 (1953).

Alazopeptin CAS Registry Number: 1397-84-8 丙氨肽霉素

Additional Names: L-Alanyl-(6-diazo-5-oxo)-L-norleucyl-(6-diazo-5-oxo)-L-norleucine
Percent Composition: C 49.45%, H 5.53%, N 23.07%, O 21.96%
Literature References: Tumor-inhibiting antibiotic produced by Streptomyces griseoplanus from soil near Williamsburg, Iowa: De Voe et al., Antibiot. Annu. 1956-7, p 730. Peptide consisting of one mole a-alanine and two moles of a C6 diazo keto amino acid oxidizable to glutamic acid: E. L. Patterson et al., Antimicrob. Agents Chemother. 1965, 115-118. Anti-tumor activity: T. Hata et al., J. Antibiot. 26, 181 (1973). Toxicity: J. B. Thiersch, Proc. Soc. Exp. Biol. Med. 97, 888 (1958).

Thalicarpine CAS Registry Number: 5373-42-2 唐松草碱

CAS Name: (6aS)-9-[4,5-Dimethoxy-2-[[(1S)-1,2,3,4-tetrahydro-6,7-dimethoxy-2-methyl-1-isoquinolinyl]methyl]phenoxy]-5,6,6a,7-tetrahydro-1,2,10-trimethoxy-6-methyl-4H-dibenzo[de,g]quinoline
Perc...
Literature References: Tumor-inhibitory alkaloid from Thalictrum dasycarpum Fisch. Lall., Ranunculaceae: Kupchan et al., J. Pharm. Sci. 52, 985 (1963). Structure: Kupchan, Yokoyama, J. Am. Chem. Soc. 86, 2177 (1964); Tomita et al., Tetrahedron Lett. 1965, 4309. Total synthesis: Kupchan, Liepa, Chem. Commun. 1971, 599; Kupchan et al., J. Am. Chem. Soc. 95, 2995 (1973). Pharmacology: Herman, Chadwick, Toxicol. Appl. Pharmacol. 26, 137 (1973); S. M. Sieber et al., Cancer Treat. Rep. 60, 1127 (1976). Antimicrobial and hypotensive activity: W. N. Wu et al., Lloydia 40, 508 (1977). Biosynthesis: D. S. Bhakuni, S. Jain, Tetrahedron 38, 729 (1982).

Tetramethylsilane CAS Registry Number: 75-76-3 四甲基硅烷

Additional Names: TMS; silicon tetramethyl
Percent Composition: C 54.46%, H 13.71%, Si 31.84%
Literature References: Two crystalline forms exist, a and b; b form is more stable. Prepn and properties: E. Krause, A. von Grosse in Die Chemie der metall-organischen Verbindungen, (Gebrüder Borntraeger, Berlin, 1937) pp 258-262; J. G. Aston et al., J. Am. Chem. Soc. 63, 2343 (1941); S. Tannenbaum et al., ibid. 75, 3753 (1953). Dielectric properties: A. P. Altshuller, L. Rosenblum, ibid. 77, 272 (1955). Temperature dependence of magnetic susceptibility, 1H, and 13C chemical shifts: F. G. Morin et al., J. Magn. Reson. 48, 138 (1982). Thermodynamic properties: W. V. Steele, J. Chem. Thermodynam. 15, 595 (1983). Use in chemical vapor deposition of films of silicon carbide, q.v.: N. Herlin et al., J. Phys. Chem. 96, 7063 (1992); A. Grill, V. Patel, J. Appl. Phys. 85, 3314 (1999). Definition of 1H resonance of TMS as the NMR primary standard: R. K. Harris et al., Pure Appl. Chem. 73, 1795 (2001).

Benzoin Oxime CAS Registry Number: 441-38-3 α-安息香肟

CAS Name: 2-Hydroxy-1,2-diphenylethanone oxime
Additional Names: 2-hydroxy-2-phenylacetophenone oxime
Percent Composition: C 73.99%, H 5.77%, N 6.16%, O 14.08%
Literature References: Two isomers occur: a or anti and b or syn. Both have been prepd from benzoin and hydroxylamine hydrochloride. Prepn of a-form: Werner, Detscheff, Ber. 38, 69 (1905); F. J. Welcher, Organic Analytical Reagents vol. III (Van Nostrand, New York, 1947) pp 239-251. Prepn of b-form: Werner, Detscheff, loc. cit. Configuration of a- and b-forms: Meisenheimer, Meis, Ber. 57, 289 (1924).

Sunitinib CAS Registry Number: 557795-19-4 舒尼替尼

CAS Name: N-[2-(Diethylamino)ethyl]-5-[(Z)-(5-fluoro-1,2-dihydro-2-oxo-3H-indol-3-ylidene)methyl]-2,4-dimethyl-1H-pyrrole-3-carboxamide
Additional Names: 5-[5-fluoro-2-oxo-1,2-dihydroindol-(3Z)...
Literature References: Tyrosine kinase inhibitor targeting VEGF-R2, PDGF-Rb, KIT and FLT3. Prepn: P. C. Tang et al., WO 0160814 (2001 to Sugen); eidem, US 6573293 (2003 to Sugen; Pharmacia Upjohn); and kinase inhibition activity: L. Sun et al., J. Med. Chem. 46, 1116 (2003). Pharmacology: D. B. Mendel et al., Clin. Cancer Res. 9, 327 (2003). Clinical pharmacokinetics and evaluation in acute myeloid leukemia: A.-M. O'Farrell et al., ibid. 5465. LC-MS-MS determn in biological samples: S. Barattè et al., J. Chromatogr. A 1024, 87 (2004). Formulation development: A. Sistla et al., Drug Dev. Ind. Pharm. 30 19 (2004). Review of development and therapeutic potential: K. M. Sakamoto, Curr. Opin. Invest. Drugs 5, 1329-1339 (2004).