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

s-Trioxane CAS Registry Number: 110-88-3 三聚甲醛

CAS Name: 1,3,5-Trioxane
Additional Names: 1,3,5-trioxacyclohexane; metaformaldehyde; trioxymethylene
Percent Composition: C 40.00%, H 6.71%, O 53.28%
Literature References: Review: Walker, Carlisle, Chem. Eng. News 21, 1250 (1943).

Rhod-2 CAS Registry Number: 132523-91-2

CAS Name: 9-[4-[Bis(carboxymethyl)amino]-3-[2-[2-[bis(carboxymethyl)amino]-5-methylphenoxy]ethoxy]phenyl]-3,6-bis(dimethylamino)xanthylium chloride
Percent Composition: C 60.72%, H 5.48%, Cl 4....
Literature References: Rhodamine-based calcium specific fluorescent dye. Prepn: R. Y. Tsien, A. Minta, EP 314480; eidem, US 5049673 (1989, 1991 both to Univ. California); A. Minta et al, J. Biol. Chem. 264, 8171 (1989). Use in monitoring intramitochondrial Ca2+: M. Hoth, R. S. Lewis in Imaging Neurons, R. Yuste et al., Eds. (Cold Spring Harbor Laboratory Press, Cold Spring Harbor, NY, 2000) pp 1-14; in free/intracellular Ca2+ levels: M.-P. Muriel et al., J. Comp. Neurol. 426, 297 (2000); G. A. MacGowan et al., J. Biomed. Opt. 6, 23 (2001).

Nisin CAS Registry Number: 1414-45-5 乳酸链球菌素

CAS Name: Nisin A
Trademarks: Nisaplin (Aplin Barrett); Novasin (Danisco)
Percent Composition: C 51.21%, H 6.91%, N 17.54%, O 17.65%, S 6.69%
Literature References: Ribosomally synthesized antimicrobial peptide produced by Lactococcus lactis (formerly Streptococcus lactis); name derived from "group N inhibitory substance". Member of the class I bacteriocins known as lantibiotics; structure contains 34 amino acid residues, eight of which are rarely found in nature, including lanthionine, q.v., and b-methyllanthionine. Isoln and antibacterial activity: A. T. R. Mattick, A. Hirsch, Nature 154, 551 (1944); eidem, Lancet 250, 417 (1946); 253, 5 (1947). Purification and nature of nisin: N. J. Berridge et al., Biochem. J. 52, 529 (1952). Production: H. B. Hawley, R. H. Hall, US 2935503 (1960 to Aplin Barrett). Structure: E. Gross, J. L. Morrell, J. Am. Chem. Soc. 93, 4634 (1971). Confirmation of structure of nisin and its major degradation product: M. Barber et al., Experientia 44, 266 (1988). Partial synthesis: K. Fukase et al., Bull. Chem. Soc. Jpn. 59, 2505 (1986). Total synthesis: K. Fukase et al., Tetrahedron Lett. 29, 795 (1988). Biosynthetic study: G. W. Buchman et al., J. Biol. Chem. 263, 16260 (1988). Review of properties and commercial applications: A. Hurst, D. G. Hoover, Food Sci. Technol. 57, 369-394 (1993); J. Delves-Broughton et al., Antonie van Leeuwenhoek 69, 193-202 (1996); of biosynthesis: C.-I. Cheigh, Y.-R. Pyun, Biotechnol. Lett. 27, 1641-1648 (2005); of biosynthesis, mode of action and comparison with other lantibiotics: C. Chatterjee et al., Chem. Rev. 105, 633-683 (2005).

Rilmazafone CAS Registry Number: 99593-25-6 利马扎封

CAS Name: 5-[[(Aminoacetyl)amino]methyl]-1-[4-chloro-2-(2-chlorobenzoyl)phenyl]-N,N-dimethyl-1H-1,2,4-triazole-3-carboxamide
Additional Names: 1-(2-o-chlorobenzoyl-4-chlorophenyl)-5-glycylamino...
Literature References: Ring-opened triazolobenzodiazepine derivative. Prepn: K. Hirai, H. Sugimoto, DE 2725164; eidem, US 4159374 (1977, 1979 both to Shionogi); and CNS activity: K. Hirai et al., J. Heterocycl. Chem. 19, 1363 (1982). Receptor binding study of rilmazafone and its closed ring active metabolites: M. Fujimoto et al., Biochem. Pharmacol. 33, 1645 (1984). Combined HPLC determn and enzyme immunoassay in plasma: G. Kominami et al., J. Chromatogr. 417, 216 (1987). Series of articles on teratogenicity studies: Oyo Yakuri 30, 749-833 (1985), C.A. 104, 81885h-81887k; 102328w (1986).

Closantel CAS Registry Number: 57808-65-8 氯氰碘柳胺

CAS Name: N-[5-Chloro-4-[(4-chlorophenyl)cyanomethyl]-2-methylphenyl]-2-hydroxy-3,5-diiodobenzamideTrademarks: Flukiver (Janssen); Seponver (Ethnor)
Percent Composition: C 39.85%, H 2.13%, Cl 1...
Literature References: Salicylanilide derivative. Prepn: M. A. C. Janssen, V. K. Sipido, BE 839481; eidem, US 4005218 (1976, 1977 both to Janssen). Effectiveness against Taenia pisiformis in rabbits: R. A. F. Chevis et al., Vet. Parasitol. 7, 333 (1980); against Ancylostoma caninum: J. Guerrero et al., J. Parasitol. 68, 616 (1983); against Fasciola hepatica in sheep: B. E. Stromberg et al., ibid. 70, 446 (1984). Prolonged effect on Haemonchus contortus in sheep: C. A. Hall et al., Res. Vet. Sci. 31, 104 (1981). Acts by uncoupling oxidative phosphorylation: H. Van den Bossche et al., Arch. Int. Physiol. Biochim. 87, 851 (1979); H. J. Kane et al., Mol. Biochem. Parasitol. 1, 347 (1980).

Fosfosal CAS Registry Number: 6064-83-1 2-(膦酸氧基)苯甲酸

CAS Name: 2-(Phosphonooxy)benzoic acid
Additional Names: salicylic acid dihydrogen phosphate; o-carboxyphenyl phosphate; salicyl phosphateTrademarks: Disdolen (Uriach)
Percent Composition: C...
Literature References: Salicylic acid deriv. Prepn: A. C. Marin Moga, E. Francia Barra, DE 2641526 (1978 to Uriach), C.A. 88, 136317h (1978). Pharmacology and comparison with aspirin: J. Garcia Rafanell et al., Arzneim.-Forsch. 30, 1091 (1980). Toxicity studies: M. S. Sanchez et al., ibid. 1098. Pharmacokinetics: V. Rimbau et al., Arch. Farmacol. Toxicol. 7, 61 (1981). Double-blind trials in musculoskeletal/articular pain: C. Diaz et al., Clin. Ther. 4, 121 (1981); L. Madera Cat, J. Garcia Rafanell, Med. Clin. 76, 18 (1981).

Cupric Sulfate, Basic CAS Registry Number: 1332-14-5 硫酸,铜(2+)盐,碱性的

CAS Name: Copper hydroxide sulfate
Additional Names: cupric subsulfate
Trademarks: Basi-Cop; Cuproxat (Agrolinz)
Literature References: Salts of variable compositions of cupric sulfate and cupric hydroxide or oxide. Occurs in nature as the mineral dolerophane, CuSO4.CuO. Reviews: Frear, Chemistry of the Pesticides (Van Nostrand, New York, 3rd ed., 1955) pp 316-323; idem, Agricultural Chemistry vol. 2 (Van Nostrand, New York, 1951) pp 524-525; Gmelins, Copper (8th ed.) 60B, 579-589 (1958). See also Burgundy Mixture.

Lafutidine CAS Registry Number: 118288-08-7 拉呋替丁

CAS Name: 2-[(2-Furanylmethyl)sulfinyl]-N-[(2Z)4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-butenyl]-acetamide
Additional Names: 2-(furfurylsulfinyl)-N-[(Z)-4-[[4-(piperidinomethyl)-2-pyridyl...
Literature References: Second generation histamine H2-receptor antagonist. Prepn of racemate: N. Hirakawa et al., EP 282077; eidem, US 4912101 (1988, 1990 both to Fujirebio); and pharmacology: eidem, Chem. Pharm. Bull. 46, 616 (1998). Pharmacology: S. Onodera et al., Jpn. J. Pharmacol. 68, 161 (1995). Mode of action study: M. Umeda et al., J. Gastroenterol. Hepatol. 14, 859 (1999). Gastroprotective effects in rats: H. Ajioka et al., Pharmacology 61, 83 (2000). Clinical pharmacokinetics: S. Haruki et al., Yakuri to Chiryo 23, 3049 (1995). Toxicology study: A. Broadmeadow et al., Oyo Yakuri 50, 167 (1995).

Amprenavir CAS Registry Number: 161814-49-9 安普那韦

CAS Name: [(1S,2R)-3-[[(4-Aminophenyl)sulfonyl](2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic acid (3S)-tetrahydro-3-furanyl ester
Additional Names: 4-amino-N-((2syn,3S)-2-hyd...
Literature References: Second generation HIV protease inhibitor. Prepn: R. D. Tung et al., WO 9405639; eidem, US 5585397 (1994, 1996 both to Vertex). Crystal structure of complex with HIV protease: E. E. Kim et al., J. Am. Chem. Soc. 117, 1181 (1995). Review of design strategy: M. A. Navia et al., Int. Antiviral News 3, 143-145 (1995); of pharmacology and clinical evaluation: J. C. Adkins, D. Faulds, Drugs 55, 837-842 (1998).

Darunavir CAS Registry Number: 206361-99-1 地瑞拉韦

CAS Name: [(1S,2R)-3-[[(4-Aminophenyl)sulfonyl] (2-methylpropyl)amino]-2-hydroxy-1-(phenylmethyl)propyl]carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester
Additional Names: (1S,2R,...
Literature References: Second generation HIV-1 protease inhibitor; structurally similar to amprenavir, q.v. Prepn: A. K. Ghosh et al., Bioorg. Med. Chem. Lett. 8, 687 (1998); idem et al., J. Org. Chem. 69, 7822 (2004). See also: J. W. Erickson, S. V. Gulnik, WO 9967417 (1999 to U.S. Dept. Health Human Serv.); J. W. Erickson et al., US 05158713 (2005 to Univ. Illinois). In vitro activity vs multidrug resistant HIV isolates: Y. Koh et al., Antimicrob. Agents Chemother. 47, 3123 (2003). Crystal structures of complex with protease variants: Y. Tie et al., J. Mol. Biol. 338, 341 (2004). Structure activity study and pharmacokinetic analysis: D. L. N. G. Surleraux et al., J. Med. Chem. 48, 1813 (2005). Review of pharmacology and clinical experience: A. C. Shurtleff, Curr. Opin. Invest. Drugs 5, 879-886 (2004). Clinical evaluation of combination with ritonavir: K. Arastéh et al., AIDS 19, 943 (2005).