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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

Picromycin CAS Registry Number: 19721-56-3 白丝菌素

Additional Names: (E)-14-Ethyl-13-hydroxy-3,5,7,9,13-pentamethyl-6-[[3,4,6-trideoxy-3-(dimethylamino)-b-D-xylo-hexopyranoside]oxy]oxacyclotetradec-11-ene-2,4,10-trione; pikromycin; albomycetin; am...
Literature References: First macrolide antibiotic isolated. Isoln from Actinomyces spp by Lindenbein and Bauer, see Brockmann, Henkel, Naturwissenschaften 37, 138 (1950); Ber. 84, 284 (1951); Brockmann, Bohne, US 2693433 (1954 to Schenley). Structure: Brockmann, Oster, Ber. 90, 605 (1957); Anliker, Gubler, Helv. Chim. Acta 40, 119, 1768 (1957). Studies in stereochemistry: Djerassi, Halpern, J. Am. Chem. Soc. 79, 3926 (1957); Ogura et al., ibid. 97, 1930 (1975); eidem, Tetrahedron 37, Suppl. 1, 165 (1981). Revised structure: Rickards, Smith, Chem. Commun. 1968, 1049; Muxfeldt et al., J. Am. Chem. Soc. 90, 4748 (1968). Synthesis from narbonolide: Maezawa et al., J. Antibiot. 26, 771 (1973).

Phosphinothricin CAS Registry Number: 35597-44-5 [(3S)-3-氨基-4-羟基-4-氧代丁基]-(羟基甲基)-氧代鏻

CAS Name: (2S)-2-Amino-4-(hydroxymethylphosphinyl)butanoic acid
Additional Names: 2-ammonio-4-methylphosphinicobutyrate; L-PPT
Percent Composition: C 33.15%, H 6.68%, N 7.73%, O 35.33%, P 17...
Literature References: First natural L-amino acid containing a phosphinic acid group. Isolated from the tripeptide antibiotic, bialaphos; inhibits glutamine synthetase. Isoln from S. viridochromogenes and synthesis of DL-form: E. Bayer et al., Helv. Chim. Acta 55, 224 (1972). Synthesis of DL-form: H. Gross, T. Gnauk, J. Prakt. Chem. 318, 157 (1976); of enantiomers: N. Minowa et al., Tetrahedron Lett. 25, 1147 (1984). Crystal structure: E. F. Paulus, S. Grabley, Z. Kristallogr. 160, 63 (1982). Determn in biological fluids: A. Suzuki, M. Kawana, Bull. Environ. Contam. Toxicol. 43, 17 (1989). Environmental impact in lakes: M. J. Faber et al., Environ. Toxicol. Chem. 17, 1291 (1998). Field trial in orchards and vineyards as herbicide: P. Langelüddeke et al., Meded. Fac. Landbouwwet. Rijksuniv. Gent 47, 95 (1982); on seed potato as desiccant: H. M. Lawson, J. S. Wiseman, Brighton Crop Prot. Conf. - Weeds 1991, 233. Review of syntheses, activities and uses: G. Hoerlein, Rev. Environ. Contam. Toxicol. 138, 73-145 (1994).

Epibatidine CAS Registry Number: 140111-52-0 (±)-三色素蛙素

CAS Name: (1R,2R,4S)-2-(6-Chloro-3-pyridinyl)-7-azabicyclo[2.2.1]heptane
Percent Composition: C 63.31%, H 6.28%, Cl 16.99%, N 13.42%
Literature References: First naturally occurring non-opioid, organochlorine, alkaloid analgesic; isolated from skin of the Ecuadoran poison frog, Epipedobates tricolor. Isoln and structural determn: T. F. Spande et al., J. Am. Chem. Soc. 114, 3475 (1992). First natural product identified which contains the 7-azabicyclo[2.2.1]heptane ring system. Synthesis of (±)-form: C. A. Broka, Tetrahedron Lett. 1993, 3251.

Androstane-3 b ,11 b -diol-17-one CAS Registry Number: 514-17-0 5-A-雄烷-3-B-11-B-二醇-17-酮*晶体

CAS Name: (3b,5a,11b)-3,11-Dihydroxyandrostan-17-one
Percent Composition: C 74.47%, H 9.87%, O 15.66%
Literature References: First obtained by degradation of allopregnane-3b,11b,17a,20b,21-pentol (Reichstein's Substance A): Reichstein, Helv. Chim. Acta 19, 402 (1936), but later isolated in small quantities directly from extracts of the adrenal cortex: Reichstein, von Euw, ibid. 21, 1197 (1938); ibid. 24, 879 (1941). It is uncertain whether this substance occurs in the fresh adrenal gland; it may possibly occur by oxidation or decompn during the isolation procedure: Reichstein, Shoppee, Vitam. Horm. I, 368 (1943). Structure-activity study: S. Sassa et al., J. Biol. Chem. 254, 10011 (1979). Chromatographic studies: A. Kerebel et al., J. Chromatogr. 140, 229 (1977); J. T. Lin, E. Heftmann, ibid. 237, 215 (1982).

Digitalose CAS Registry Number: 4481-08-7

CAS Name: 6-Deoxy-3-O-methylgalactose
Additional Names: 3-methyl-D-fucose
Percent Composition: C 47.19%, H 7.92%, O 44.90%
Literature References: First obtained by Kiliani, Ber. 25, 2116 (1892), by hydrolysis of Digitalinum verum, a glycoside of gitoxigenin with glucose and digitalose. By hydrolysis of a glycoside from the seeds of Strophanthus eminii Aschers Pax., Apocynaceae: Lamb, Smith, J. Chem. Soc. 1936, 442. Configuration: Schmidt et al., Naturwissenschaften 31, 247 (1943); Ann. 555, 26 (1944). Elderfield in Advances in Carbohydrate Chemistry vol. I (New York, 1945) p 150. Prepn by isoln and hydrolysis of emicymarin from Strophanthus eminii seeds: Elderfield, ibid. 156. Synthesis: Reber, Reichstein, Helv. Chim. Acta 29, 343 (1946). Schmidt, Wernicke, Ann. 558, 70 (1947).

Captopril CAS Registry Number: 62571-86-2 卡托普利

CAS Name: 1-[(2S)-3-Mercapto-2-methyl-1-oxopropyl]-L-proline
Additional Names: (2S)-1-(3-mercapto-2-methylpropionyl)-L-proline; D-2-methyl-3-mercaptopropanoyl-L-prolineTrademarks: Acediur (Guid...
Literature References: First orally active angiotensin-converting enzyme (ACE) inhibitor. Prepn: M. A. Ondetti, D. W. Cushman, DE 2703828; eidem, US 4046889 and US 4105776 (1977, 1977, 1978 all to Squibb). Design and synthesis: M. A. Ondetti et al., Science 196, 441 (1977); D. W. Cushman et al., Biochemistry 16, 5484 (1977). Improved synthesis: D. H. Nam et al., J. Pharm. Sci. 73, 1843 (1984). Pharmacology: B. Rubin et al., Eur. J. Pharmacol. 51, 377 (1978); eidem, Prog. Cardiovasc. Dis. 21, 183 (1978). Clinical studies: D. B. Case et al., ibid. 195; H. R. Brunner et al., Ann. Intern. Med. 90, 19 (1979). Toxicology and metabolism: G. R. Keim in Captopril and Hypertension, D. B. Case, Ed. (Plenum, New York, 1980) p 137. GC/MS determn in biological fluids: T. Ito, Y. Matsuki, J. Chromatogr. 417, 79 (1987). Historical review and comprehensive bibliography: Z. P. Horovitz in Pharmacological and Biochemical Properties of Drug Substances vol. 3, M. E. Goldberg, Ed. (Am. Pharm. Assoc., Washington, DC, 1981) pp 148-175. Comprehensive description: H. Kadin, Anal. Profiles Drug Subs. 11, 79-137 (1982). Reviews: Am. Heart J. 104, pt. 2, 1125-1228 (1982); Br. J. Clin. Pharmacol. 14, Suppl. 2, 69S-252S (1982). Series of articles on pharmacology and therapeutic efficacy: Postgrad. Med. J. 62, Suppl. 1, 1-191 (1986).

Methylene Blue CAS Registry Number: 61-73-4 亚甲基蓝

CAS Name: 3,7-Bis(dimethylamino)phenothiazin-5-ium chloride
Additional Names: C.I. Basic Blue 9; methylthioninium chloride; tetramethylthionine chloride; 3,7-bis(dimethylamino)phenazathionium c...
Literature References: First prepd by Caro in 1876. Provided technically as the zinc double chloride; used medically in a zinc free form. Prepn: H. E. Fierz-David, L. Blangey, Fundamental Processes of Dye Chemistry (Interscience, New York, 1949) p 311. See also Colour Index vol. 4 (3rd ed., 1971) p 4470. TLC determn: G. Balansard et al., Ann. Pharm. Fr. 46, 129 (1988). Use as marker for reticulocytes: B. Rudensky, Scand. J. Clin. Lab. Invest. 57, 291 (1997); in melanoma targeted radiotherapy: E. M. Link et al., Pigment Cell Res. 7, 358 (1994); P. J. Blower et al., Nucl. Med. Biol. 24, 305 (1997). Review of use as vital dye: P. Barbosa, T. M. Peters, Histochem. J. 3, 71-93 (1971). History and properties: R. D. Lillie, P. T. Donaldson, Stain Technol. 54, 33-39 (1979). Review of photochemistry: E. M. Tuite, J. M. Kelly, J. Photochem. Photobiol. B 21, 103-124 (1993). Review of use as cationic dye in ceramic quality control: J. E, Funk, D. R. Dinger in Science of Whitewares, V. E. Henkes et al., Eds. (American Ceramic Society, OH, 1996) pp 21-31. Review of use in methemoglobinaemia: J. W. Harvey, A. S. Keitt, Br. J. Haematol. 54, 29-41 (1983).

Thiolactic Acid CAS Registry Number: 79-42-5 硫代乳酸

CAS Name: 2-Mercaptopropanoic acid
Additional Names: 2-mercaptopropionic acid; 2-thiolpropionic acid; a-mercaptopropanoic acid
Percent Composition: C 33.95%, H 5.70%, O 30.15%, S 30.21%
Literature References: First prepd from a-chloropropionic acid and potassium hydrosulfide: Schacht, Ann. 129, 3 (1864); prepn from a-chloropropionic acid and sodium thiosulfate: Martin, US 2413361 (1946 to Martin Labs). From sodium sulfide, sulfur and a-bromopropionic acid: Dumesnil, US 2985557 (1961 to Frank E. Jonas). Review: Reid, Organic Chemistry of Bivalent Sulfur vol. I (Chemical Publ. Co., New York, 1958) p 449.

Papain CAS Registry Number: 9001-73-4 木瓜蛋白酶

Additional Names: Papayotin; vegetable pepsin
Trademarks: Arbuz; Nematolyt; Summetrin; Tromasin; Velardon (Organon); Vermizym
Literature References: First recognized member of the class of proteolytic enzymes that needs a free sulfhydryl group for activity. Isolated from the latex of the green fruit and leaves of Carica papaya L., Caricaceae. Initial isolation and crystallization: Balls et al., Science 86, 379 (1937); Balls, Lineweaver, J. Biol. Chem. 130, 669 (1939). Prepn from commercial dried papaya latex and physical properties: Kimmel, Smith, ibid. 207, 515 (1954); see also ibid. 533-573; Becker, Econ. Bot. 12, 62 (1958). Purification: Gibian, Bratfisch, US 2950227 (1960 to Schering AG); Lesuk, US 3011952 (1961 to Sterling Drug); Blumberg et al., Eur. J. Biochem. 15, 97 (1970). The papain molecule consists of one folded polypeptide chain of 212 residues, mol wt ~23,400. Complete amino acid sequence: Drenth et al., Nature 218, 929 (1968); Mitchel et al., J. Biol. Chem. 245, 3485 (1970). Mechanism of action studies: Morihara, J. Biochem. 62, 250 (1967). Use in treatment of contact lenses to prolong wearing time in keratoconic patients with papillary conjunctivitis: D. R. Korb et al., Arch. Ophthalmol. 101, 48 (1983). Reviews: Kimmel, Smith in Adv. Enzymol. Relat. Subj. Biochem. 19, 267-334 (1957); Glazer, Smith in The Enzymes vol. III, P. D. Boyer, Ed. (Academic Press, New York, 3rd ed., 1971) pp 501-537; see also Drenth et al., ibid. 485-498 and eidem, Adv. Protein Chem. 25, 79-115 (1971) for a comprehensive review of the structural elucidation.

Dacarbazine CAS Registry Number: 4342-03-4 达卡巴嗪

CAS Name: 5-(3,3-Dimethyl-1-triazenyl)-1H-imidazole-4-carboxamide
Additional Names: 5(or 4)-(dimethyltriazeno)imidazole-4(or 5)-carboxamide; DIC; DTICTrademarks: Dacatic (L×kefarmos); DTIC-Dome...
Literature References: First synthesized in 1959 at the Southern Research Institute. Prepn: Shealy et al., J. Org. Chem. 27, 2150 (1962); Hano et al., Gann 59, 207 (1968), C.A. 69, 42527g (1968). Antitumor activity: Shealy et al., Biochem. Pharmacol. 11, 674 (1962); Hano et al., Gann 56, 417 (1965), C.A. 63, 18856g (1965). Mechanism of action studies: Saunders, Schultz, Biochem. Pharmacol. 19, 911 (1970). Metabolism: Skibba et al., ibid. 2043; Mizuno, Humphrey, Cancer Chemother. Rep. Part 1 56, 465 (1972). Review: Carter, Friedman, Eur. J. Cancer 8, 85-92 (1972), see also the series of articles on history, activity, mechanism of action and clinical studies: Cancer Treat. Rep. 60, 123-214 (1976).