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

Emitefur CAS Registry Number: 110690-43-2 乙嘧替氟

CAS Name: 3-[[3-(Ethoxymethyl)-5-fluoro-3,6-dihydro-2,6-dioxo-1(2H)-pyrimidinyl]carbonyl]benzoic acid 6-(benzoyloxy)-3-cyano-2-pyridinyl ester
Additional Names: 3-[3-(6-benzoyloxy-3-cyano-2-pyr...
Literature References: Bifunctional prodrug composed of a derivative of 5-fluorouracil (5-FU) and 3-cyano-2,6-dihydroxypyridine (CNDP), an inhibitor of 5-FU degradation by dihydrouracil dehydrogenase. Prepn: S. Fujii, DE 3709699; idem, US 4983609 (1988, 1991 both to Otsuka); M. Hirohashi et al., Chem. Pharm. Bull. 41, 1498 (1993). Antitumor activity: S. Fujii et al., Jpn. J. Cancer Res. 80, 173 (1989). Mechanism of action: T. Okayasu et al., ibid. 85, 101 (1994). Clinical evaluation in lung cancer: Y. Nakai et al., Acta Oncol. 33, 523 (1994). Toxicity study: H. Kinoshita et al., Yakuri to Chiryo 22, 81 (1994), C.A. 121, 99197 (1994).

Colestilan CAS Registry Number: 95522-45-5 考来替兰

CAS Name: 2-Methyl-1H-imidazole polymer with (chloromethyl)oxirane
Additional Names: 2-methylimidazole polymer with 1-chloro-2,3-epoxypropane; colestimideTrademarks: Cholebine (Mitsubishi)
Literature References: Bile acid sequestering anion exchange resin. Prepn: H. Toda, K. Kihara, JP Kokai 59138228 (1984 to Mitsubishi Petrochem.); and bile acid binding activity: H. Toda et al., J. Pharm. Sci. 77, 531 (1988). Series of articles on pharmacology and toxicology: Jpn. Pharmacol. Ther. 24, Suppl. 4, 1-181 (1996). Clinical evaluation in type II hyperlipoproteinemia: Y. Homma et al., Nutr. Metab. Cardiovasc. Dis. 6, 211 (1996); in hyperphosphatemia: S. Kurihara et al., Nephrol. Dial. Transplant. 20, 424 (2005).

Levosimendan CAS Registry Number: 141505-33-1 左西孟旦

CAS Name: [[4-[(4R)-1,4,5,6-Tetrahydro-4-methyl-6-oxo-3-pyridazinyl]phenyl]hydrazono]propanedinitrile
Additional Names: (-)-[p[(R)-1,4,5,6-tetrahydro-4-methyl-6-oxo-3-pyridazinyl]phenyl]hydrazo...
Literature References: Bioactive enantiomer of racemate, simendan. Positive inotropic agent with vasodilating activity. Binds to and sensitizes the myocardial contractile protein, troponin C, to calcium, thereby stabilizing the troponin conformation needed to trigger muscle contraction. Prepn: R. J. Backstrom et al., GB 2251615; P. Nore et al., US 5569657 (1992, 1996 both to Orion). Pharmacology: A. F. E. Rump et al., Pharmacol. Toxicol. 74, 244 (1994). Binding studies: P. Pollesello et al., J. Biol. Chem. 269, 28584 (1994). HPLC determn in plasma: M. Karlsson et al., Biomed. Chromatogr. 11, 54 (1997). Clinical pharmacokinetics: E.-P. Sandell et al., J. Cardiovasc. Pharmacol. 26, Suppl. 1, S57 (1995). Review of mechanism of action: H. Haikala, I.-B. Lindén, ibid., S10-S19 (1995); of pharmacology, toxicology and clinical evaluation: P. S. Pagel et al., Cardiovasc. Drug Rev. 14, 286-316 (1996). Comparison with dobutamine, q.v., in heart failure: F. Follath et al., Lancet 360, 196 (2002).

Norelgestromin CAS Registry Number: 53016-31-2 甲基孕酮

CAS Name: (17a)-13-Ethyl-17-hydroxy-18,19-dinorpregn-4-en-20-yn-3-one oxime
Additional Names: 17-deacetylnorgestimate; 18-methylnorethindrone oxime; levonorgestrel 3-oximePercent Composition: C...
Literature References: Bioactive metabolite of norgestimate, q.v. Prepd as intermediate of norgestrel, q.v.: NL 7306609 (1973 to Richter Gedeon). Prepn and identification as norgestimate metabolite: S. F. Sisenwine et al., Contraception 15, 25 (1977). Pharmacology: J. L. McGuire et al., Am. J. Obstet. Gynecol. 163, 2127 (1990). Use as contraceptive patch: J. Jona et al., WO 9640355; eidem, US 5876746 (1996, 1999 both to Cygnus). Clinical pharmacokinetics: L. S. Abrams et al., Br. J. Clin. Pharmacol. 53, 141 (2002). Review of clinical pharmacology and efficacy: R. T. Burkman, Int. J. Fertil. 47, 69-76 (2002); B. L. Sicat, Pharmacotherapy 23, 472-480 (2003).

Honokiol CAS Registry Number: 35354-74-6 和厚朴酚

CAS Name: 3',5-Di-2-propenyl-[1,1'-biphenyl]-2,4'-diol
Additional Names: 3',5-diallyl-2,4'-biphenyldiol; 5,3'-diallyl-2,4'-dihydroxydiphenyl
Percent Composition: C 81.17%, H 6.81%, O 12.01%
Literature References: Bioactive principle isolated from the bark of Magnolia obovata, Thunb., Magnoliaceae and other Magnolia species used in Japanese and Chinese traditional medicine. Name derived from "Honoki", the Japanese name of M. obovata. Isomeric with magnolol, q.v. Identification in methanolic extracts of M. obovata bark: M. Fujita et al., Chem. Pharm. Bull. 20, 212 (1972). Isoln from seeds of M. grandiflora L.: F. S. El-Feraly, W.-S. Li, Lloydia 41, 442 (1978). Synthesis: T. Takeya et al., Chem. Pharm. Bull. 34, 2066 (1986). CNS depressant effects in vivo: K. Watanabe et al., Planta Med. 49, 103 (1983). HPLC determn in M. officinalis extracts: T.-H. Tsai, C.-F. Chen, J. Chromatogr. 598, 143 (1992).

Tacalcitol CAS Registry Number: 57333-96-7 他卡西妥

CAS Name: (1a,3b,5Z,7E,24R)-9,10-Secocholesta-5,7,10(19)-triene-1,3,24-triol
Additional Names: 1a,24(R)-dihydroxycholecalciferol; 1a,24R-dihydroxyvitamin D3Trademarks: Bonealfa (Teijin); Curato...
Literature References: Bioactive, synthetic vitamin D3 analog; exhibits antiproliferative effect on keratinocytes. Prepn: T. Takeshita et al., DE 2526981; eidem, US 4022891 (1976, 1977 both to Teijin); M. Morisaki et al., J. Chem. Soc. Perkin Trans. 1 1975, 1421; K. Ochi et al., ibid. 1979, 165. Pharmacology: T. Matsunaga et al., J. Dermatol. 17, 135 (1990). Clinical evaluation in psoriasis: M. J. P. Gerritsen et al., Br. J. Dermatol. 131, 57 (1994). Review: M. Nishimura et al., Eur. J. Dermatol. 3, 255-261 (1993).

Sodium Ferric Gluconate CAS Registry Number: 34089-81-1 复合葡萄糖酸钠铁注射剂

CAS Name: D-Gluconic acid iron(3+) sodium salt
Literature References: Bioavailable iron supplement containing a ferric hydroxide core stabilized and solubilized by simple carbohydrates. Prepn: W. Traube et al., Ber. 66B, 1545 (1933). Intestinal absorption of clinical formulations: L. Samochowiec, Clin. Ter. 56, 341 (1971).

a -Terthienyl CAS Registry Number: 1081-34-1 alpha-三联噻吩

CAS Name: 2,2':5'2''-Terthiophene
Additional Names: 5-(2-thienyl)-2,2'-bithiophene
Percent Composition: C 58.03%, H 3.25%, S 38.73%
Literature References: Biocidal constituent of various species of marigolds. Isoln from Tagetes erecta L., Compositae: L. Zechmeister, J. W. Sease, J. Am. Chem. Soc. 69, 273 (1947). Isoln and distribution in Tageteae: K. R. Downum, G. H. N. Towers, J. Nat. Prod. 46, 98 (1983). Synthesis: W. Steinkopf et al., Ann. 546, 180 (1941); H. J. Kooreman, H. Wynberg, Rec. Trav. Chim. 86, 37 (1967); J.-P. Beny et al., J. Org. Chem. 47, 2201 (1982). Biological activity as nematocide: J. H. Uhlenbroek, J. D. Bijloo, Rec. Trav. Chim. 77, 1004 (1958); J. D. Bijloo et al., DE 1075891; eidem, US 3050442 (1960, 1962, both to North American Philips); J. Bakker et al., J. Biol. Chem. 254, 1841 (1979); as herbicide: J. Harvey, Jr., US 3086854 (1963 to Du Pont); G. Campbell et al., J. Chem. Ecol. 8, 961 (1982); as antimicrobial: J. R. Kagan et al., Photochem. Photobiol. 31, 465 (1980); T. Arnason et al., ibid. 33, 821 (1981); F. DiCosmo et al., Pestic. Sci. 13, 589 (1982).

Paclitaxel Poliglumex CAS Registry Number: 263351-82-2 聚谷氨酸紫杉醇

CAS Name: (1R,2S)-2-(Benzoylamino)-1-[[[(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-6,12b-bis(acetyloxy)-12-(benzoyloxy)-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl...
Literature References: Biodegradable polymer drug conjugate resulting from the random condensation of L-polyglutamic acid and paclitaxel, q.v., which has on average 10.4 monomeric glutamic acid units per paclitaxel-glutamate conjugate unit. Mol wt ~48 kDa. Prepn: C. Li et al., Cancer Res. 58, 2404 (1998). See also: eidem, US 5977163 (1999 to PG-TXL Co.). In vitro activities in comparison with paclitaxel: A. S. Multani et al., Anticancer Res. 17, 4269 (1997); E. A. Oldham et al., Int. J. Oncol. 16, 125 (2000). Irradiation enhanced tumor specificity: C. Li et al., Clin. Cancer Res. 6, 2829 (2000); L. Milas et al., Int. J. Radiat. Oncol. Biol. Phys. 55, 707 (2003). Review of properties and preclinical characterization: J. W. Singer et al., Adv. Exp. Med. Biol. 519, 81-99 (2003); of clinical development: J. W. Singer, J. Controlled Rel. 109, 120-126 (2005); M. Man, H. Rugo, IDrugs 8, 739-754 (2005).

Lactic Acid Homopolymer CAS Registry Number: 26023-30-3; 26161-42-2 ( L -form); 26917-25-9 ( D -form) 聚[氧(1-甲基-2-氧代-1,2-乙二基)]

CAS Name: Poly[oxy(1-methyl-2-oxo-1,2-ethanediyl)]
Additional Names: poly(lactic acid); PLA
Trademarks: EcoPLA (Cargill Dow); Lacea (Mitsui Toatsu); Lactron (Kanebo); Lacty (Shimadzu)
Literature References: Biodegradable thermoplastic polymer which can be derived from entirely renewable resources; degrades in vivo to lactic acid. Prepn: W. H. Carothers et al., J. Am. Chem. Soc. 54, 761 (1932); J. Kleine, H.-H. Kleine, Makromol. Chem. 30, 23 (1959). Synthesis of L-form by lactide ring-opening polymerization: H. R. Kricheldorf, S.-R. Lee, Polymer 36, 2995 (1995); by lactic acid melt/solid polycondensation: R. Miyoshi et al., Int. Polym. Process. 11, 320 (1996); S.-I. Moon et al., High Perform. Polym. 13, S189 (2001). Kinetics and mechanism of ring-opening polymerization: W. Dittrich, R. C. Schulz, Angew. Makromol. Chem. 15, 109 (1971). Comparison of properties from different synthetic methods: M. Ajioka et al., J. Environ. Polym. Degrad. 3, 225 (1995). Comparison of melt-spun and solution-spun L-form fibers: B. Eling et al., Polymer 23, 1587 (1982). Thermal properties: K. Jamshidi et al., ibid. 29, 2229 (1988). 13C solid state NMR study of crystallinity and morphology: K. A. M. Thakur et al., Macromolecules 29, 8844 (1996). 1H NMR determn of lactide composition: idem et al., Anal. Chem. 69, 4303 (1997). Study to assess potential use in surgical implants: R. K. Kulkarni et al., Arch. Surg. 93, 839 (1966). Brief reviews: M. Matsui, Chem. Fibers Int. 46, 318-319 (1996); M. Dartee et al., ibid. 50, 546, 548, 551 (2000). Review of properties and uses: M. Vert et al., J. Macromol. Sci.-Pure Appl. Chem. A32, 787-796 (1995); of material design systems: M. Spinu et al., ibid. A33, 1497-1530 (1996); of biocompatibility and clinical orthopaedic applications: K. A. Athanasiou et al., Biomaterials 17, 93-102 (1996); of mfr, properties and commercial applications: J. Lunt, Polym. Degrad. Stab. 59, 145-152 (1998); of use in drug delivery with polyglycolide: R. A. Jain, ibid. 21, 2475-2490 (2000).