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

Hyalobiuronic Acid CAS Registry Number: 499-15-0 2-氨基-2-脱氧-3-O-beta-D-吡喃葡糖基-alpha-D-吡喃葡萄糖

CAS Name: 2-Amino-2-deoxy-3-O-b-D-glucopyranuronosyl-D-glucose
Additional Names: 3-O-(b-D-glucopyranosyluronic acid)-2-amino-2-deoxy-D-glucose
Percent Composition: C 40.57%, H 5.96%, N 3.94%...
Literature References: Disaccharide unit of hyaluronic acid. Isoln from hyaluronic acid: Rapport et al., Nature 168, 996 (1951). Structure: Weissman, Meyer, J. Am. Chem. Soc. 76, 1753 (1954). Synthesis: Takanashi et al., ibid. 84, 3029 (1962).

Rose Bengal CAS Registry Number: 632-68-8 孟加拉玫瑰红B

CAS Name: 4,5,6,7-Tetrachloro-3',6'-dihydroxy-2',4',5',7'-tetraiodospiro[isobenzofuran-1(3H),9'-[9H]xanthen]-3-one dipotassium salt
Additional Names: 4,5,6,7-tetrachloro-2',4',5',7'-tetraiodofl...
Literature References: Discovered by Gnehm 1882; tetraiodinate of 4,5,6,7-tetrachlorofluorescein (from resorcinol and tetrachlorophthalic anhydride) converted to potassium salt: Colour Index vol. 4 (3rd ed., 1971) 4428. Labeling with 131I: Liebster, Andrysek, Nature 184, 913 (1959). See also: H. J. Conn's Biological Stains, R. D. Lillie, Ed., (Williams Wilkins, Baltimore, 9th ed., 1977) p 350. Diagnostic use in hepatic function: K. S. Nijran, D. C. Barber, Phys. Med. Biol. 31, 563 (1986).

Quinizarin Green SS CAS Registry Number: 128-80-3 1,4-双(对甲苯基氨基)蒽-9,10-二酮

CAS Name: 1,4-Bis[(4-methylphenyl)amino]-9,10-anthracenedione
Additional Names: 1,4-di-p-toluidinoanthraquinone; D C Green No. 6; C.I. Solvent Green 3; C.I. 61565
Percent Composition: C 80....
Literature References: Discovered by R. E. Schmidt in 1894: Colour Index vol. 4 (3rd ed., 1971) p 4541.

Suramin Sodium CAS Registry Number: 129-46-4 舒拉明钠

CAS Name: 8,8'-[Carbonylbis[imino-3,1-phenylenecarbonylimino(4-methyl-3,1-phenylene)carbonylimino]]bis-1,3,5-naphthalenetrisulfonic acid hexasodium salt
Additional Names: hexasodium sym-bis(m-a...
Literature References: Discovered in 1917 by O. Dressel and R. Kothe: J. Dressel, J. Chem. Educ. 38, 620 (1961). Prepn: E. Fourneau et al., Compt. Rend. 178, 675 (1924); J. Trefouel, E. Fourneau, GB 224849 (1923); B. Heymann, Angew. Chem. 37, 585 (1924). Pharmacology, toxicology and clinical antiparasitic activity: F. Hawking, Adv. Pharmacol. Chemother. 15, 289-322 (1978). Inhibition of reverse transcriptase in vitro: E. De Clercq, Cancer Lett. 8, 9 (1979); vs HIV: H. Mitsuya et al., Science 226, 172 (1984). HPLC determn in plasma: R. W. Klecker, J. M. Collins, J. Liq. Chromatogr. 8, 1685 (1985). Pharmacokinetics: J. M. Collins et al., J. Clin. Pharmacol. 26, 22 (1986). Pharmacology and virustatic effect in AIDS: S. Broder et al., Lancet 2, 627 (1985); A. M. Levine et al., Ann. Intern. Med. 105, 32 (1986). Clinical trial in onchocerciasis: H. Schultz-Key et al., Trop. Med. Parasitol. 36, 244 (1985); in prostate cancer: C. Myers et al., J. Clin. Oncol. 10, 881 (1992). Review: Olenick in Antibiotics vol. 3, J. W. Corcoran, F. E. Hahn, Eds. (Springer-Verlag, New York, 1975) pp 699-703; R. La Rocca et al., Cancer Cells 2, 106-115 (1990).

Bucillamine CAS Registry Number: 65002-17-7 布西拉明

CAS Name: N-(2-Mercapto-2-methyl-1-oxopropyl)-L-cysteine
Additional Names: N-(2-mercapto-2-methylpropanoyl)-L-cysteine; N-(2-mercaptoisobutyryl)-L-cysteine; tiobutarit; thiobutaritTrademarks: R...
Literature References: Disease modifying antirheumatic drug (DMARD) which modulates the immune response; structurally related to tiopronin, q.v. Prepn: T. Fujita et al., DE 2709820; eidem, US 4305958 (1977, 1981 both to Santen); M. Oya et al., Chem. Pharm. Bull. 29, 940 (1981). GC-MS determn in blood: K. Matsuura et al., J. Mass Spectrom. Soc. Jpn. 46, 25 (1998). Clinical immunopharmacology: H. Matsuno et al., Drugs Exp. Clin. Res. 19, 205 (1993). Clinical trials in rheumatoid arthritis: M. Yasuda et al., Clin. Rheumatol. 13, 446 (1994); H. A. Kim, Y. W. Song, Rheumatol. Int. 17, 5 (1997).

Lobenzarit CAS Registry Number: 63329-53-3 2-((2-羧基苯基)氨基)-4-氯苯甲酸

CAS Name: 2-[(2-Carboxyphenyl)amino]-4-chlorobenzoic acid
Additional Names: N-(2-carboxyphenyl)-4-chloroanthranilic acid; 4-chloro-2,2'-iminodibenzoic acid; CCA
Percent Composition: C 57.65%...
Literature References: Disease modifying antirheumatic drug (DMARD) with immunomodulating activity. Prepn: M. Tanemura et al., DE 2526092; eidem, US 4092426 (1976, 1978 both to Chugai). HPLC determn in plasma: F. J. Schwende, S. W. Turner, Pharm. Res. 8, 523 (1991). Immunosuppression of B cell activity: S. Hirohata et al., Arthritis Rheum. 35, 168 (1992). Clinical trial in rheumatoid arthritis: Y. Shiokawa et al., J. Rheumatol. 11, 615 (1984); in systemic lupus erythematosus: S. Hirohata et al., Clin. Exp. Rheumatol. 12, 261 (1994). Review of pharmacology: R. González, D. Remirez, Invest. Allergol. Clin. Immunol. 7, 77-82 (1997).

Leflunomide CAS Registry Number: 75706-12-6 来氟米特

CAS Name: 5-Methyl-N-[4-(trifluoromethyl)phenyl]-4-isoxazolecarboxamide
Additional Names: a,a,a-trifluoro-5-methyl-4-isoxazolecarboxy-p-toluidide; 5-methylisoxazole-4-carboxylic acid trifluorom...
Literature References: Disease modifying antirheumatic drug (DMARD) with immunosuppressant activity. Converted in vivo to its active open ring metabolite, teriflunomide, q.v. Inhibits de novo pyrimidine biosynthesis in immune cells. Prepn: F. J. Kaemmerer, R. Schleyerbach, DE 2854439; eidem, US 4284786 (1980, 1981 both to Hoechst); and pharmacology: P. Fossa et al., Farmaco 46, 789 (1991). HPLC determn of active metabolite in plasma: V. C. Dias et al., Ther. Drug Monit. 17, 84 (1995). Review of mechanisms of action: R. I. Fox, J. Rheumatol. 25, Suppl. 53, 20-26 (1998); of clinical pharmacology: B. Rozman, ibid. 27-32. Clinical trial in rheumatoid arthritis: V. Strand et al., Arch. Intern. Med. 159, 2542 (1999). Reviews: C. Miceli-Richard, M. Dougados, Expert Opin. Pharmacother. 4, 987-997 (2003); J. P. Kaltwasser, F. Behrens, ibid. 6, 787-801 (2005).

Gold Sodium Thiomalate CAS Registry Number: 12244-57-4 金(I)硫丁二酸钠

CAS Name: Mercaptobutanedioic acid monogold(1+) sodium salt
Additional Names: sodium aurothiomalate
Trademarks: Myochrysine (Merck Co.); Shiosol (Shionogi); Tauredon (Byk Gulden)
Literature References: Disease modifying antirheumatic drug (DMARD). Mixture of the mono- (C4H4AuNaO4S) and disodium (C4H3AuNa2O4S) salts of gold thiomalic acid. Prepn as the monohydrate of the disodium salt: M. Delépine, US 1994213 (1935 to Rhone Poulenc). Detection in blood by atomic absorption spectroscopy: A. I. A. Rodgers et al., Anal. Proc. 19, 87 (1982). Clinical pharmacokinetics: K. L. N. Blocka et al., Clin. Pharmacokinet. 11, 133 (1986). Discussion of mechanisms of action: H. A. Capell, Agents Actions Suppl. 24, 158 (1988). Clinical trial in rheumatoid arthritis: R. Munro et al., Ann. Rheum. Dis. 57, 88 (1998).

Aurothioglucose CAS Registry Number: 12192-57-3 葡糖硫金

CAS Name: (1-Thio-D-glucopyranosato-O2,S1)gold
Additional Names: (1-D-glucosylthio)gold; gold thioglucose
Trademarks: Aureotan (Byk Gulden); Solganal (Schering)
Percent Composition: C 18....
Literature References: Disease modifying antirheumatic drug (DMARD). Prepn: Lebeau-Janot, Traité Pharm. Chim. II, 661 (1956). Induction of obesity in exptl animals: A. F. Debons et al., Fed. Proc. 36, 143 (1977). Clinical comparison with auranofin, q.v., in rheumatoid arthritis: P. L. C. M. Van Riel et al., Clin. Rheumatol. 5, 359 (1986); P. E. Prete et al., Clin. Rheumatol. 13, 60 (1994).

Pantethine CAS Registry Number: 16816-67-4 D-泛硫乙胺

CAS Name: N,N'-[Dithiobis[2,1-ethanediylimino(3-oxo-3,1-propanediyl)]]bis[2,4-dihydroxy-3,3-dimethylbutanamide]
Additional Names: N,N'-[dithiobis(ethyleneiminocarbonylethylene)]bis(2,4-dihydrox...
Literature References: Disulfide dimer of pantetheine, q.v. Growth factor for Lactobacillus bulgaricus: Williams et al., J. Biol. Chem. 177, 933 (1949). Formed by oxidation of pantetheine: Brown, Snell, J. Biol. Chem. 198, 375 (1952). Structure: Snell et al., J. Am. Chem. Soc. 72, 5349 (1950). Synthesis: Wieland, Bokelmann, Naturwissenschaften 38, 384 (1951); Wittle et al., J. Am. Chem. Soc. 75, 1694 (1953); Viscontini et al., Helv. Chim. Acta 37, 375 (1954); Bowman, Cavalla, J. Chem. Soc. 1954, 1171; Shimizu et al., Chem. Pharm. Bull. 13, 180 (1965). Clinical trial in hyperlipoproteinemia: A. Gaddi et al., Atherosclerosis 50, 73 (1984).