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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

Anisomycin CAS Registry Number: 22862-76-6 茴香霉素

CAS Name: (2R,3S,4S)-2-[(4-Methoxyphenyl)methyl]-3,4-pyrrolidinediol 3-acetate
Additional Names: [2R-(2a,3a,4b)]-2-[(4-methoxyphenyl)methyl]-3,4-pyrrolidinediol 3-acetate; 2-p-methoxyphenylmeth...
Literature References: Protein synthesis inhibiting antibiotic isolated from Streptomyces: B. A. Sobin, F. W. Tanner, Jr., J. Am. Chem. Soc. 76, 4053 (1954); Tanner et al., US 2691618 (1954 to Pfizer). Activity: J. E. Lynch et al., Antibiot. Chemother. 4, 844, 899 (1954). Structure and stereochemistry: J. J. Beereboom et al., J. Org. Chem. 30, 2334 (1965); J. P. Schaefer, P. J. Wheatley, ibid. 33, 166 (1968); K. Butler, ibid. 2136. Biosynthesis: idem, ibid. 31, 317 (1966). Total synthesis: Oida, Ohki, Chem. Pharm. Bull. 16, 2086 (1968); ibid. 17, 1405 (1969); I. Felner, K. Schenker, Helv. Chim. Acta 53, 754 (1970). Chiral synthesis: J. P. H. Verheyden et al., Pure Appl. Chem. 50, 1363 (1978). Stereospecific total synthesis: D. P. Schumacher, S. S. Hall, J. Am. Chem. Soc. 104, 6076 (1982). Improved synthesis: A. N. Hulme, E. M. Rosser, Org. Lett. 4, 265 (2002). Mechanism of action: A. Jiménez, D. Vázquez in Antibiotics vol. 5(pt. 2), F. E. Hahn, Ed. (Springer-Verlag, New York, 1979) pp 1-19. Soly and stability data: Antibiot. Annu. 1954-55, pp 809-810. Memory impairment effects in mice: K. M. Lattal, T. Abel, Proc. Natl. Acad. Sci. USA 101, 4667 (2004).

Sparsomycin CAS Registry Number: 1404-64-4 司帕索霉素

CAS Name: (2E)-N-[(1S)-1-(Hydroxymethyl)-2-[(R)-[(methylthio)methyl]sulfinyl]ethyl]-3-(1,2,3,4-tetrahydro-6-methyl-2,4-dioxo-5-pyrimidinyl)-2-propenamide
Additional Names: (E)-(1S)-1,2,3,4-tetr...
Literature References: Protein synthesis inhibitor with antibiotic and antitumor activity. Isoln from fermentation broth of Streptomyces sparsogenes var sparsogenes: S. P. Owen et al., Antimicrob. Agents Chemother. 1962, 772; GB 974541 (1964 to Upjohn); from S. cuspidosporus: E. Higashide et al., Takeda Kenkyusho Nempo 25, 1 (1966), C.A. 66, 54238q (1967). Characterization and purification: A. D. Argoudelis, R. R. Herr, Antimicrob. Agents Chemother. 1962, 780. Structural elucidation: P. F. Wiley, F. A. MacKellar, J. Org. Chem. 41, 1858 (1976). Total synthesis: H. C. J. Ottenheijm et al., ibid. 46, 3273 (1981); R. M. J. Liskamp et al., ibid. 5408. HPLC determn in plasma and urine: B. Winograd et al., J. Chromatogr. 275, 145 (1983). Pharmacokinetics and toxicology: Z. Zylicz et al., Cancer Chemother. Pharmacol. 20, 115 (1987). Ribosomal binding studies: E. Lazaro et al., Antimicrob. Agents Chemother. 35, 10 (1991). Biosynthetic studies: R. J. Parry et al., J. Am. Chem. Soc. 114, 5946 (1992). Review of chemistry and biological activity: H. C. J. Ottenheijm et al., Prog. Med. Chem. 23, 220-268 (1986).

PSK® (Kureha) CAS Registry Number: 66455-27-4 α1-酸性糖蛋白来源于人类血浆

Trademarks: KRESTIN (Kureha)
Literature References: Protein-bound polysaccharide; biological response modifier having immunostimulant and anticancer properties. Isolated from a basidiomycete, Coriolus versicolor (Fr.) Quel.: S. Otsuka et al., JP 73 8489 (1973 to Kureha), C.A. 80, 41025g (1974). Antitumor activity: S. Tsukagoshi et al., Prog. Chemother. (Antibacterial, Antiviral, Antineoplast.), Proc. Int. Congr. Chemother., 8th, Athens 1973 vol. 3, G. K. Daikos, Ed. (Hellen. Soc. Chemother., Athens, 1974) pp 799-803. Clinical studies as postoperative immunotherapy: M. Torisu et al., Cancer Immunol. Immunother. 31, 261 (1990); Y. Kuroda et al., Int. J. Clin. Oncol. 3, 311 (1998). Review: S. Tsukagoshi et al., Cancer Treat. Rev. 11, 131-155 (1984). Review of antimicrobial and biological activity: H. Sakagami, M. Takeda in Mushroom Biology and Mushroom Products (Chinese Univ. Press, Hong Kong, 1993) p 237-245; antimetastatic effects: H. Kobayashi et al., Cancer Epidemiol. Biomarkers Prev. 4, 275-281 (1995).

Bromelain CAS Registry Number: 9001-00-7 菠萝蛋白酶

Trademarks: Bromelin; Ananase (Rorer); Extranase (Rorer); Inflamen (Hokuriku); Traumanase (Rorer)
Literature References: Protein-digesting and milk-clotting enzymes found in pineapple fruit juice and stem tissue. Enzymes from the two sources are distinguished as fruit bromelain and stem bromelain. First isolns of fruit bromelain: Marcano, Bull. Pharm. 5, 77 (1891); Chittenden, Trans. Conn. Acad. Sci. 8, 281 (1892). From pineapple juice by precipitation with acetone and also with ammonium sulfide: Heinicke, US 3002891 (1961 to Pineapple Res. Inst.). Discovery in stem tissue: idem, Science 118, 753 (1953). Stem bromelain has mol wt of about 33,000 and is probably the first proteolytic enzyme of plant origin to be established as a glycoprotein: Murachi et al., Biochemistry 3, 48 (1964); Ota et al., ibid. 180. Purification of crude prepns: Gibian, Bratfisch, US 2950227 (1960 to Schering AG). Reviews: Balls et al., Ind. Eng. Chem. 33, 950 (1941); of stem bromelain: Murachi, "Structure and Function of Stem Bromelain," in Proteins, Structure and Function vol. 2, M. Funatsu et al., Eds. (Kodansha, Tokyo, Wiley, New York, 1972) pp 47-101.

Thermolysin CAS Registry Number: 9073-78-3 嗜热菌蛋白酶

Additional Names: Bacillus thermoproteolyticus neutral proteinase; EC 3.4.24.27
Literature References: Proteolytic enzyme of mol wt 37,500 that hydrolyzes protein bonds on the N-terminal side of hydrophobic amino acid residues. Contains a zinc atom essential for activity and four Ca2+ ions essential for thermal and conformational stability. Isoln from Bacillus thermoproteolyticus: S. Endo, J. Ferment. Technol. 40, 346 (1962). Properties and amino acid composition: Y. Ohta et al., J. Biol. Chem. 241, 5919 (1966). Site of enzymatic hydrolysis: Y. Ohta, Y. Ogura, J. Biochem. 58, 607 (1965). Substrate specificity studies: H. Matsubara et al., Biochem. Biophys. Res. Commun. 21, 242 (1965); 24, 427 (1966); K. Morihara, H. Tsuzuki, Biochim. Biophys. Acta 118, 215 (1966). Stability studies: Y. Ohta, J. Biol. Chem. 242, 509 (1967). Inhibition studies: H. Matsubara et al., Biochem. Biophys. Res. Commun. 34, 719 (1969); J. Murphy et al., Arch. Biochem. Biophys. 202, 405 (1980). Purification: H. Matsubara, Methods Enzymol. 19, 642 (1970). Structure studies: K. Titani et al., Nature 238, 35 (1972); B. W. Matthews et al., ibid. 37, 41; P. M. Colman et al., J. Mol. Biol. 70, 701 (1972). Function of the metal ions: J. Feder et al., Biochemistry 10, 4552 (1971); G. Voordouw, R. S. Roche, ibid. 14, 4667 (1975); R. S. Roche, G. Voordouw, Crit. Rev. Biochem. 5, 1 (1978). Effect of the histidyl residue on the mechanism of action: S. Blumberg et al., Isr. J. Chem. 12, 643 (1974); M. K. Pangburn, K. A. Walsch, Biochemistry 14, 4050 (1975). Review: Experientia 26, Suppl., 31-59 (1976).

Chymopapain CAS Registry Number: 9001-09-6 糜木瓜酶

Trademarks: Chymodiactin (Smith); Discase (Boots)
Literature References: Proteolytic enzyme which is the major component of the crude latex of Carica papaya, Caricaceae. A sulfhydryl enzyme similar to papain, q.v., with respect to substrate specificities, but differing in electrophoretic mobility, stability and solubility. Original crystallization and partial characterization: Jansen, Balls, J. Biol. Chem. 137, 459 (1941); eidem, US 2313875 (1943). Consists of four components, two of which have molecular wts of about 35,000 and have been isolated and studied. Chymopapain A: Erbata, Yasunobu, J. Biol. Chem. 237, 1086 (1962); chymopapain B: Kunimitsu, Yasunobu, Biochim. Biophys. Acta 139, 405 (1966); Isunoda, Yasunobu, J. Biol. Chem. 241, 4610 (1966). Purification: Stern, US 3558433 (1971 to Baxter Labs.). Specificity studies: Ebata, Takahashi, Biochim. Biophys. Acta 118, 201 (1966). Reviews: Kunimitsu, Yasunobu, Methods Enzymol. 19, 244-252 (1970); Glazer, Smith, The Enzymes vol. III, P. D. Boyer, Ed. (Academic Press, New York, 3rd ed., 1971) pp 537-538. Review of use in herniated disk treatment: M. J. David, J. Am. Med. Assoc. 243, 2043 (1980).

Worenine CAS Registry Number: 38763-29-0 甲基黄连碱

CAS Name: 5,6-Dihydro-14-methylbis[1,3]benzodioxolo[5,6-a:5',6'-g]quinolizinium
Additional Names: 13-methyl-y-coptisine
Literature References: Protoberberine alkaloid isolated from root of Coptis japonica Makino, Ranunculaceae: Kitasato, J. Pharm. Soc. Jpn. No. 542, 48, 315 (1927); Acta Phytochim. 3, 175 (1927), C.A. 22, 1779-1780 (1928); in Coptis chinensis Franch., Ranunculaceae: Schramm, Wej-ds, Pharmazie 14, 405 (1959). Synthesis of 13-methyl-y-coptisine and its probable identity with worenine: T. R. Govindachari et al., Indian J. Chem. 9, 1313 (1971).

Oxadiargyl CAS Registry Number: 39807-15-3 炔丙恶唑草

CAS Name: 3-[2,4-Dichloro-5-(2-propynyloxy)phenyl]-5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2(3H)-one
Additional Names: 5-tert-butyl-3-(2,4-dichloro-5-propargyloxyphenyl)-1,3,4-oxadiazol-2-(3H)-on...
Literature References: Protoporphyrinogen IX oxidase inhibitor; pre-emergence herbicide for use in rice and other food crops. Prepn: R. Boesch, DE 2227012; idem, US 3818026 (1972, 1974 both to Rhone-Poulenc). Properties and field trials: R. Dickmann et al., Brighton Crop Prot. Conf. - Weeds 1997, 51; G. Tracchi et al., ibid. 885.

Verapamil CAS Registry Number: 52-53-9 维拉帕米

CAS Name: a-[3-[[2-(3,4-Dimethoxyphenyl)ethyl]methylamino]propyl]-3,4-dimethoxy-a-(1-methylethyl)benzeneacetonitrile
Additional Names: 5-[(3,4-dimethoxyphenethyl)methylamino]-2-(3,4-dimethoxyph...
Literature References: Prototype calcium antagonist; vasodilating activity resides primarily in the (S)-isomer. Both isomers inhibit the p-glycoprotein efflux pump in multidrug resistant tumor cells. Prepn: BE 615861; Dengel, US 3261859 (1962, 1966 both to Knoll). Pharmacology: H. Haas, G. Härtfelder, Arzneim.-Forsch. 12, 549 (1962). Physical and chemical data: W. Appel, ibid. 562. Synthesis and absolute configuration of enantiomers: H. Ramuz, Helv. Chim. Acta 58, 2050 (1975). Stereospecific synthesis: L. J. Theodore, W. L. Nelson, J. Org. Chem. 52, 1309 (1987). HPLC determn of enantiomers and metabolites in plasma: G. Stagni, W. R. Gillespie, J. Chromatogr. B 667, 349 (1995). Comprehensive description: Z. L. Chang, Anal. Profiles Drug Subs. 17, 643-674 (1988). Review of pharmacology and therapeutic use in arrhythmias: B. N. Singh et al., Drugs 25, 125-153 (1983); in hypertension: D. McTavish, E. M. Sorkin, ibid. 38, 19-76 (1989). Clinical trial of dexverapamil as adjunct to cancer chemotherapy: G. Kornek et al., Cancer 76, 1356 (1995); R. J. Motzer et al., J. Clin. Oncol. 13, 1958 (1995).

Sulfamidochrysoidine CAS Registry Number: 103-12-8 磺胺米柯定

CAS Name: 4-[(2,4-Diaminophenyl)azo]benzenesulfonamide
Additional Names: 2,4-diaminoazobenzene-4'-sulfonamide; 4'-sulfamyl-2,4-diaminoazobenzene
Percent Composition: C 49.47%, H 4.50%, N 24....
Literature References: Prototype compd leading to the development of sulfonamide antibacterials. Prepn: F. Mietzsch, J. Klarer, DE 607537 (1935 to I. G. Farbenind.); eidem, US 2085037 (1937 to Winthrop). Antibacterial activity in vivo: G. Domagk, Dtsch. Med. Wochenschr. 61, 573 (1935); (for English translation see Rev. Infect. Dis. 8, 163 (1986)). Identification of sulfanilamide as active metabolite: J. Tréfouel et al., C.R. Seances Soc. Biol. Ses Fil. 120, 756 (1935); L. Colebrook et al., Lancet 2, 1323 (1936). Polymorphic forms in commercial prepns: L. Kofler, A. Kofler, Monatsh. Chem. 81, 321 (1950). Use to visualize carbonic anhydrase during isoelectric focusing in polyacrylamide gels: W. Siffert et al., J. Biochem. Biophys. Methods 8, 331 (1983). Historical review: M. H. Bickel, Gesnerus 45, 67-86 (1988).