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

Tranexamic Acid CAS Registry Number: 1197-18-8 凝血酸,氨甲环酸

CAS Name: trans-4-(Aminomethyl)cyclohexanecarboxylic acid
Additional Names: AMCHATrademarks: Anvitoff (Abbott); Cyklokapron (Pfizer); Exacyl (Sanofi-Synthelabo); Spiramin (Mitsui); Spotof (CCD)...
Literature References: Antifibrinolytic agent; blocks lysine binding sites of plasminogen. Prepn: A. Einhorn, C. Ladisch, Ann. 310, 194 (1900); M. Levine, R. Sedlecky, J. Org. Chem. 24, 115 (1959); NL 6503605; T. Naito et al., US 3499925 (1965, 1970 to both Daiichi Seiyaku and Mitsubishi Chem.). Pharmacology: Andersson et al., Scand. J. Haematol. 2, 230 (1965). Resoln of isomers and antiplasmin activity: M. Shimizu et al., Chem. Pharm. Bull. 16, 357 (1968), T. Naito et al., ibid., 728. Toxicity data: B. Melander et al., Acta Pharmacol. Toxicol. 22, 340 (1965). Clinical study in treatment of acute upper gastrointestinal tract bleeding: D. Barer et al., N. Engl. J. Med. 308, 1571 (1983); in menorrhagia: J. Bonnar, B. L. Sheppard, Br. Med. J. 313, 579 (1996). Review of pharmacology and therapeutic use: C. J. Dunn, K. L. Goa, Drugs 57, 1005-1032 (1999).

e -Aminocaproic Acid CAS Registry Number: 60-32-2 6-氨基己酸

CAS Name: 6-Aminohexanoic acid
Additional Names: epsilon-aminocaproic acid; epsilcapramin; EACATrademarks: Amicar (Wyeth); Epsikapron (Pharmacia); Hemocaprol (Sanofi-Aventis)
Percent Composi...
Literature References: Antifibrinolytic; inhibits the activity of plasmin and plasminogen, q.q.v. Prepn: S. Gabriel, T. A. Maass, Ber. 32, 1266 (1899); A. Galat, S. Mallin, J. Am. Chem. Soc. 68, 2729 (1946); C. Y. Meyers, L. E. Miller, Org. Synth. coll. vol. IV, 39 (1963). Toxicity data: D. W. Hallesy et al., Pharmacologist 3, 62 (1961). Crystal structure: G. Bodor et al., Acta Crystallogr. 23, 482 (1967). Clinical trial and mode of action study: T. J. Vander Salm et al., J. Thorac. Cardiovasc. Surg. 112, 1098 (1996).

Nolatrexed CAS Registry Number: 147149-76-6 诺拉曲特

CAS Name: 2-Amino-6-methyl-5-(4-pyridinylthio)-4(1H)-quinazolinone
Additional Names: 2-amino-3,4-dihydro-6-methyl-4-oxo-5-(4-pyridylthio)quinazoline; 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)-3...
Literature References: Antifolate thymidylate synthase inhibitor. Prepn: S. E. Webber et al., WO 9320055; eidem, US 5707992 (1993, 1998 both to Agouron); S. E. Webber et al., J. Med. Chem. 36, 733 (1993). Solid-state properties: A. K. Dash, P. Tyle, J. Pharm. Sci. 85, 1123 (1996). Pharmacology: S. Webber et al., Cancer Chemother. Pharmacol. 37, 509 (1996). Clinical pharmacokinetics: I. Rafi et al., Clin. Cancer Res. 1, 1275 (1995). Clinical evaluation in hepatocellular carcinoma: K. Stuart et al., Cancer 86, 410 (1999).

Wortmannin CAS Registry Number: 19545-26-7 渥曼青霉素

CAS Name: (1S,6bR,9aS,11R,11bR)-11-(Acetyloxy)-1,6b,7,8,9a,10,11,11b-octahydro-1-(methoxymethyl)-9a,11b-dimethyl-3H-furo[4,3,2-de]indeno[4,5-h]-2-benzopyran-3,6,9-trione
Percent Composition: C ...
Literature References: Antifungal antibiotic from Penicillium wortmanni Klocker: Brian et al., Trans. Br. Mycol. Soc. 40, 365 (1957). Similar to viridin, q.v. Structure: MacMillan et al., Chem. Commun. 1968, 613; eidem, J. Chem. Soc. Perkin Trans. 1 1972, 2898. Absolute stereochemistry: Petcher et al., Chem. Commun. 1972, 1061; MacMillan et al., ibid. 1063.

Cerulenin CAS Registry Number: 17397-89-6 浅蓝菌素

CAS Name: (2R,3S)-3-[(4E,7E)-1-Oxo-4,7-nonadienyl]oxiranecarboxamide
Additional Names: 2,3-epoxy-4-oxo-7,10-dodecadienamide; 2,3-epoxy-4-oxo-7,10-dodecadienoylamide; helicocerin
Percent Comp...
Literature References: Antifungal antibiotic isolated from Cephalosporium caerulens; Acryocylindrium oryzae; Helicoceras oryzae: T. Hata et al., Jpn. J. Bacteriol. 15, 1075 (1960); Matsumae et al., J. Antibiot. 16A, 236, 239 (1963); Sano et al., ibid. 20A, 344 (1967); Furuya, Shirasaka, JP 70 21638 (1970 to Sankyo), C.A. 73, 108271k (1970). Biological characteristics: Matsumae et al., J. Antibiot. 17A, 1 (1964). Structure: Omura et al., ibid. 20A, 349 (1967). Abs config: eidem, Chem. Pharm. Bull. 17, 2361 (1969); Arison, Omura, J. Antibiot. 27, 28 (1974). Stereoselective synthesis of (+)- and (-)-tetrahydrocerulenin and corrected abs config of (+)-cerulenin: H. Ohrui, S. Emoto, Tetrahedron Lett. 1978, 2095; J.-R. Pougny, P. Sinay, ibid. 3301. Stereoselective synthesis of the (+)-form from D-glucose: N. Sueda et al., ibid. 1979, 2039; M. Pietraszkiewicz, P. Sinay, ibid. 4741. Interrupts yeast-type fungi growth by inhibiting the biosynthesis of sterols and fatty acids. Mechanism of action studies: Nomura et al., J. Biochem. 71, 783 (1972); eidem, J. Antibiot. 25, 365 (1972); see also D. Vance, Biochem. Biophys. Res. Commun. 48, 649 (1972). Total synthesis of (±)-cerulenin: R. K. Boeckman, Jr., E.W. Thomas, J. Am. Chem. Soc. 99, 2805 (1977); A. A. Jakubowski et al., Tetrahedron Lett. 1977, 2399; E. J. Corey, D. R. Williams, ibid. 3847; K. Mikami et al., Chem. Lett. 1981, 1721; A. A. Jakubowski et al., J. Org. Chem. 47, 1221 (1982).

Pecilocin CAS Registry Number: 19504-77-9 培西洛星

CAS Name: 1-[(2E,4E,6E,8R)-8-Hydroxy-6-methyl-1-oxo-2,4,6-dodecatrienyl]-2-pyrrolidinone
Trademarks: Supral (Basotherm); Variotin (Leo Pharm)
Percent Composition: C 70.07%, H 8.65%, N 4.81%,...
Literature References: Antifungal antibiotic isolated from Paecilomyces varioti Bainier var. antibioticus: S. Takeuchi et al., J. Antibiot. 12A, 109, 195 (1959); Sumiki et al., GB 866425 (1961 to Japan. Antibiot. Res. Assoc. and Nippon Kayaku). Structure: S. Takeuchi et al., J. Antibiot. 17A, 267 (1964). Stereochemistry: S. Takeuchi, H. Yonehara, Tetrahedron Lett. 1966, 5197. Revised structure and stereochemistry (E,Z,E to E,E,E): eidem, J. Antibiot. 22, 179 (1969). Synthesis of the dl-form: A. Ishida, T. Mukaiyama, Chem. Lett. 1977, 467; eidem, Bull. Chem. Soc. Jpn. 51, 2077 (1978).

Pyrrolnitrin CAS Registry Number: 1018-71-9 硝吡咯菌素

CAS Name: 3-Chloro-4-(3-chloro-2-nitrophenyl)pyrrole
Additional Names: 3-chloro-4-(2'-nitro-3'-chlorophenyl)pyrrole; PN
Trademarks: Pyroace (Fujisawa)
Percent Composition: C 46.72%, H 2.3...
Literature References: Antifungal antibiotic isolated from Pseudomonas pyrrocinia n. sp.: K. Arima et al., Agric. Biol. Chem. 28, 575 (1964); eidem, J. Antibiot. 18, 201 (1965). Structure: Imanaka et al., ibid. 207. Synthesis: S. Umio et al., BE 670427; eidem, US 3428648 (1964, 1969 both to Fujisawa); Nakano et al., Tetrahedron Lett. 1966, 737; S. Umio et al. (10 publications) Chem. Pharm. Bull. 17, 559-628 (1969); Gosteli, Helv. Chim. Acta 55, 451 (1972). Pharmacological studies: M. Nishida et al., J. Antibiot. 18, 211 (1965).

Albofungin CAS Registry Number: 37895-35-5

CAS Name: [1S-(1a,4a,8aa)]-13-Amino-3,4,8a,13-tetrahydro-1,15,16-trihydroxy-4-methoxy-12-methyl-1H-xantheno[4',3',2':4,5][1,3]benzodioxino[7,6-g]isoquinoline-14,17(2H,9H)-dione
Percent Composit...
Literature References: Antifungal antibiotic produced by Streptomyces albus var fungistaticus (fungatus) Solovyeva et Rudaya. Isoln procedure: Khokhlov, Liberman, Proc. Symp. Antibiotics Prague (May 1959) p 81. Structure: A. I. Gurevich et al., Tetrahedron Lett. 1972, 1751. Stereochemistry: A. I. Gurevich et al., ibid. 1974, 2801. Thought to be identical with Ba-180265 described by Liu et al., in Antimicrob. Agents Chemother. 1962, 767. Chemical and biological properties: A.I. Gurevich et al., Antibiotiki 17, 771 (1972).

Dimethomorph CAS Registry Number: 110488-70-5 烯酰吗啉

CAS Name: 4-[3-(4-Chlorophenyl)-3-(3,4-dimethoxyphenyl)-1-oxo-2-propenyl]morpholine
Additional Names: 3-(4-chlorophenyl)-3-(3,4-dimethoxyphenyl) acrylic acid morpholideTrademarks: Acrobat (BASF...
Literature References: Antifungal cinnamic acid derivative; comprised of a mixture of E- and Z- isomers. Process for prepn: J. Curtze, EP 294907; idem, US 4933449 (1988, 1990 both to Shell Int.). Comprehensive description: G. Albert et al., Brighton Crop Prot. Conf. - Pests Dis. 1988, 17-24. Mechanism of action study: P. J. Kuhn et al., Mycol. Res. 95, 333 (1991). Efficacy vs downy mildew of grapevines: T. Wicks, B. Hall, Plant Dis. 74, 114 (1990). Toxicological evaluation: G. E. Veenstra, D. E. Owen, Arch. Toxicol. 1992, Suppl 15, 113.

Dermostatin CAS Registry Number: 11120-15-3 制皮菌素

Additional Names: Viridofulvin; Dermastatin
Literature References: Antifungal polyene antibiotic mixture produced by Streptomyces viridogriseus Thirum. Comprised of about 43% Dermostatin A, C40H64O11, and 57% Dermostatin B, C41H66O11, the first hexaenes to have their structures determined. Preliminary isoln and physico-chemical studies: Bhate et al., Hind. Antibiot. Bull. 4, 159 (1962), C.A. 57, 13013d (1962); Thirumalachar, Bhate, IN 76253 (1963 to Hindustan Antibiotics), C.A. 59, 8095b (1963). Purifn: Narasimhachari et al., Hind. Antibiot. Bull. 8, 111 (1966), C.A. 65, 5301c (1966). Structural studies: Narasimhachari, Swami, Chemotherapy 13, 181 (1968). Revised structure: Pandey et al., J. Antibiot. 26, 475 (1973). Antifungal activity: Menon, Hind. Antibiot. Bull. 4, 106 (1962), C.A. 57, 5121c (1962); Gordee, Butler, J. Antibiot. 24, 561 (1971).