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

Fervenulin CAS Registry Number: 483-57-8 热诚菌素

CAS Name: 6,8-Dimethylpyrimido[5,4-e]-1,2,4-triazine-5,7-(6H,8H)-dione
Additional Names: 6,8-dimethyl-5,7-dioxo-5,6,7,8-tetrahydropyrimido[5,4-e]-as-triazine; 1,3-dimethylazalumazine; planomyci...
Literature References: Antibiotic from culture filtrates of Streptomyces fervens: Eble et al., Antibiot. Annu. 1959-1960, 227. Structure: Daves et al., J. Org. Chem. 26, 5256 (1961). Synthesis: Pfleiderer, Schündehütte, Ann. 615, 42 (1958); Daves et al., J. Am. Chem. Soc. 84, 1724 (1962); Yoneda, Nagamatsu, Bull. Chem. Soc. Jpn. 48, 2884 (1975); Taylor, Sowinski, J. Org. Chem. 40, 2321 (1975); S. Senda et al., J. Am. Chem. Soc. 99, 7358 (1977).

Streptolydigin CAS Registry Number: 7229-50-7 链霉溶菌素

CAS Name: (aS,2S,4E)-4-[(2E,4E,6R)-6-[(1R,2'R,3R,4S,5R)-1,4-Dimethylspiro[2,9-dioxabicyclo[3.3.1]non-6-ene-8,2'-oxiran]-3-yl]-1-hydroxy-4-methyl-2,4-heptadienylidene]-N,a-dimethyl-3,5-dioxo-1-[(2S...
Literature References: Antibiotic isolated from culture filtrates of Streptomyces lydicus n. sp.: Eble et al., Antibiot. Annu. 1955-1956, 893; GB 779570 (1957 to Upjohn). Structure: Rinehart et al., J. Am. Chem. Soc. 85, 4083 (1963). Stereochemistry: Duchamp et al., ibid. 95, 4077 (1973). RNA-polymerase inhibitor: Cassani et al., Nature New Biol. 230, 197 (1971). NMR studies: V. J. Lee, K. L. Rinehart, J. Antibiot. 34, 408 (1980). Toxicity study: DeBoer et al., Antibiot. Annu. 1955-1956, 886.

Spectinomycin CAS Registry Number: 1695-77-8 大观霉素

CAS Name: [2R-(2a,4ab,5ab,6b,7b,8b,9a,9aa,10ab)]-Decahydro-4a,7,9-trihydroxy-2-methyl-6,8-bis(methylamino)-4H-pyrano[2,3-b][1,4]benzodioxin-4-one
Additional Names: actinospectacin; espectinomic...
Literature References: Antibiotic isolated from fermentation broth of Streptomyces spectabilis: D. J. Mason et al., Antibiot. Chemother. 11, 118 (1961); M. E. Bergy et al., ibid. 661; M. E. Bergy, C. De Boer, US 3234092 (1966 to Upjohn). Purification and crystallization: H. K. Jahnke, US 3206360; V. J. Peters, US 3272706 (1965, 1966 both to Upjohn). Isoln and characterization: A. C. Sinclair, A. F. Winfield, Antimicrob. Agents Chemother. 1961, 503. Structure: H. Hoeksema et al., J. Am. Chem. Soc. 84, 3212 (1962); P. F. Wiley et al., ibid. 85, 2652 (1963). Solubility data: J. R. Marsh, P. J. Weiss, J. Assoc. Off. Anal. Chem. 50, 457 (1967). Stereochemistry and abs config: T. G. Cochran et al., Chem. Commun. 1972, 494. Biosynthesis: L. A. Mitscher et al., ibid. 1971, 1541; H. Otsuka et al., J. Am. Chem. Soc. 102, 6817 (1980). Enantioselective synthesis: D. R. White et al., Tetrahedron Lett. 1979, 2737; S. Hanessian, R. Roy, Can. J. Chem. 63, 163 (1985). Mechanism of action study: M. F. Brink et al., Nucleic Acids Res. 22, 325 (1994). HPLC determn in animal plasma: N. Haagsma et al., J. Chromatogr. 615, 289 (1993). Clinical pharmacokinetics: J. G. Wagner et al., Int. Z. Klin. Pharmakol. Ther. Toxikol. 1, 261 (1968). Clinical evaluation in gonorrhea: Y. H. Kouri et al., Genitourin. Med. 65, 342 (1989); in chancroid: M. Guzmán et al., Sex. Transm. Dis. 19, 291 (1992). Co-treatment with lincomycin, q.v., for footrot in sheep: C. M. Venning et al., Aust. Vet. J. 67, 258 (1990). Reviews: W. M. McCormack, M. Finland, Ann. Intern. Med. 84, 712-716 (1976); W. J. Holloway, Med. Clin. North Am. 66, 169-173 (1982).

Thiolutin CAS Registry Number: 87-11-6 硫藤黄素

CAS Name: 6-(Acetamido)-4-methyl-1,2-dithiolo[4,3-b]pyrrol-5(4H)-one
Additional Names: N-(4,5-dihydro-4-methyl-5-oxo-1,2-dithiolo[4,3-b]pyrrol-6-yl)acetamide; 3-acetamido-5-methylpyrrolin-4-one...
Literature References: Antibiotic isolated from several strains of Streptomyces albus: F. W. Tanner, Jr. et al., 118th Am. Chem. Soc. Meet. (Chicago, Sept. 1950), Abstracts of Papers, p 18A; F. W. Tanner, Jr. et al., US 2689854 (1954 to Pfizer). Characterization, similarity to aureothricin, q.v.: W. D. Celmer et al., J. Am. Chem. Soc. 74, 6304 (1952). Structure: W. D. Celmer, I. A. Solomons, ibid. 77, 2861 (1955). Total synthesis: U. Schmidt, F. Geiger, Ann. 664, 168 (1963); K. Hagio, N. Yoneda, Bull. Chem. Soc. Jpn. 47, 1484 (1974). Bactericidal, protozoicidal, fungicidal properties: H. Seneca et al., Antibiot. Chemother. 2, 357 (1952). Mode of action: A. Jimenez et al., Antimicrob. Agents Chemother. 3, 729 (1973). Inhibition of microbiological growth in beer: J. B. Bockelmann, F. B. Strandskov, US 2798811 (1957 to Schaefer Brewing Co.). Activity against soil borne pathogens: P. R. Deb, B. K. Dutta, Curr. Sci. 53, 659 (1984). As allergy inhibitor: P. Stahl et al., DE 3434562 (1986 to Boehringer, Mannheim), C.A. 105, 54609k (1986).

Fusidic Acid CAS Registry Number: 6990-06-3 夫西地酸

CAS Name: (3a,4a,8a,9b,11a,13a,14b,16b,17Z)-16-(Acetyloxy)-3,11-dihydroxy-29-nordammara-17(20),24-dien-21-oic acid
Additional Names: 3a,11a,16b-trihydroxy-29-nor-8a,9b,13a,14b-dammara-17(20),24...
Literature References: Antibiotic isolated from the fermentation broth of Fusidium coccineum; structurally similar to cephalosporin P1, q.v. Inhibits bacterial protein synthesis by interference with elongation factor G. Isoln and structure: W. O. Godtfredsen et al., Nature 193, 987 (1962); Lancet I, 928 (1962); W. O. Godtfredsen, S. Vangedal, Tetrahedron 18, 1029 (1962). Identity with ramycin: H. Vanderhaeghe et al., Nature 205, 710 (1965). Structure: D. Arigoni et al., Experientia 19, 521 (1963). Stereochemistry: W. O. Godtfredsen et al., Tetrahedron 21, 3505 (1965). Synthetic studies: W. G. Dauben et al., J. Am. Chem. Soc. 94, 8593 (1972); R. E. Ireland, U. Hengartner, ibid. 3652; M. Tanabe et al., Tetrahedron Lett. 1977, 1481. Total synthesis: W. G. Dauben et al., J. Am. Chem. Soc. 104, 303 (1982). Review of structure-activity relationships: W. von Daehne et al., Adv. Appl. Microbiol. 25, 95-146 (1979). Series of articles on pharmacology and clinical experience: Int. J. Antimicrob. Ag. 12, Suppl. 2, S1-S93 (1999). Review of use in Staphylococcus aureus infections: D. Dobie, J. Gray, Arch. Dis. Child. 89, 74-77 (2004).

Diploicin CAS Registry Number: 527-93-5 2,4,7,9-四氯-3-羟基-8-甲氧基-1,6-二甲基-11H-二苯并[b,e][1,4]二氧杂卓-11-酮

CAS Name: 2,4,7,9-Tetrachloro-3-hydroxy-8-methoxy-1,6-dimethyl-11H-dibenzo[b,e][1,4]dioxepin-11-one
Additional Names: 3,5-dichloro-6-[(3,5-dichloro-6-hydroxy-4-methoxy-o-tolyl)oxy]-4,2-cresotic...
Literature References: Antibiotic isolated from the lichen Buellia canescens (Dicks.) De Not. [Diploicia canescens (Dicks.) Massal.], Lecideaceae: Zopf, Ann. 336, 58 (1904); Nolan, Sci. Proc. R. Dublin Soc. 21, 67 (1934); Nolan et al., Chem. Ind. (London) 1935, 577; Barry, Nature 158, 131 (1946). Structure: Nolan et al., Sci. Proc. R. Dublin Soc. 24, 319 (1948). Synthesis: Ollis, ibid. 27, 161 (1956); Brown et al., Proc. Chem. Soc. London 1960, 393; Hendrickson, Ramsay, Chem. Commun. 1968, 1101; Hendrickson et al., J. Am. Chem. Soc. 94, 6834 (1972); P. D. Djura et al., J. Chem. Soc. Perkin Trans. 1 1976, 147.

Hirsutic Acid C CAS Registry Number: 3650-17-7 (1aR-(1aalpha,2beta,3Abeta,3balpha,5alpha,6aalpha,7As*))-十氢-2-羟基-3a,5-二甲基-3-亚甲基-环戊二烯并(4,5)二并环戊烯并(1,6a-b)环氧乙烯-5-羧酸

CAS Name: (1aR,2R,3aR,3bR,5S,6aR,7aS)-Decahydro-2-hydroxy-3a,5-dimethyl-3-methylenecyclopenta[4,5]pentaleno[1,6a-b]oxirene-5-carboxylic acid
Additional Names: 6b,6ab-epoxy-2,3,3aa,3b,4,5,6,6a,7...
Literature References: Antibiotic metabolite isolated from the fungus Stereum hirsutum: Heatley et al., Br. J. Exp. Pathol. 28, 35 (1947). Structure and stereochemistry: Comer et al., Chem. Commun. 1965, 310; Comer, Trotter, J. Chem. Soc. B 1966, 11; Comer et al., Tetrahedron 23, 4761 (1967). Synthesis of (±)-form: Hashimoto et al., Tetrahedron Lett. 1974, 3745; M. Yamazaki et al., Chem. Lett. 1981, 1245. Stereosynthesis: B. M. Trost et al., J. Am. Chem. Soc. 101, 1284 (1979); of (+)-form: M. Shibasaki et al., Tetrahedron Lett. 23, 5311 (1982).

Terreic Acid CAS Registry Number: 121-40-4 (-)-土曲霉酸

CAS Name: (1R)-3-Hydroxy-4-methyl-7-oxabicyclo[4.1.0]hept-3-ene-2,5-dione
Additional Names: 2-hydroxy-3-methyl-1,4-benzoquinone 5,6-epoxide; 5,6-epoxy-3-hydroxy-p-toluquinone
Percent Composi...
Literature References: Antibiotic metabolite produced by the mold Aspergillus terreus; naturally occurring as the (-)-form: Wilkins, Harris, Br. J. Exp. Pathol. 23, 166 (1942); Abraham, Florey, in H. W. Florey et al., Antibiotics vol. I (Oxford Univ. Press, New York, 1949) p 337; Kaplan et al., Antibiot. Chemother. 4, 746 (1954). Structure: Sheehan et al., J. Am. Chem. Soc. 80, 5536 (1958). Synthesis of the racemate: Rashid, Read, J. Chem. Soc. C 1967, 1323. Alternate synthesis and resolution of isomers: Sheehan, Lo, J. Med. Chem. 17, 371 (1974). Improved synthesis: A. Enhsen et al., J. Org. Chem. 55, 1177 (1990).

Lycomarasmine CAS Registry Number: 7611-43-0 N-[2-[(2-氨基-2-氧代乙基)氨基]-2-羧基乙基]-L-天冬氨酸

CAS Name: N-[2-[(2-Amino-2-oxoethyl)amino]-2-carboxyethyl]-L-aspartic acid
Trademarks: Welkstoff
Percent Composition: C 38.99%, H 5.45%, N 15.16%, O 40.40%
Literature References: Antibiotic peptide (tomato-wilting agent) produced by the fungus Fusarium lycopersici. Isoln: Plattner, Clauson-Kaas, Helv. Chim. Acta 28, 188 (1945). Structure: eidem, Experientia 1, 195 (1945); Hardegger et al., Helv. Chim. Acta 46, 60 (1963).

Prodigiosin CAS Registry Number: 82-89-3 灵菌红素

CAS Name: 4-Methoxy-5-[(5-methyl-4-pentyl-2H-pyrrol-2-ylidene)methyl]-2,2'-bi-1H-pyrrole
Additional Names: 2,2'-[3-methoxy-4'-amyl-5'-methyl-5-(2''-pyrryl)]dipyrrylmethene; prodigiosine
Perc...
Literature References: Antibiotic pigment produced by Chromobacterium prodigiosum (Serratia marcescens). Exhibits antimicrobial and cytotoxic properties. Isoln: Wrede, Hettche, Ber. 62, 2678 (1929); Lasseur, Georges, Trav. Lab. Microbiol. Fac. Pharm. Nancy 9, 47 (1936); Lasseur, Melcion, ibid. 13, 192 (1944). Purification: Morgan, Tanner, J. Chem. Soc. 1955, 3305. Structure: Wrede, Rothhaas, Z. Physiol. Chem. 226, 95 (1934). Revised structure and synthesis: H. H. Wasserman et al., J. Am. Chem. Soc. 82, 506 (1960); H. Rapoport, K. G. Holden, ibid. 5510; ibid. 84, 635 (1962); A. J. Castro et al., J. Org. Chem. 28, 857 (1963). Total synthesis and in vitro cytotoxic activity: D. L. Boger, M. Patel, Tetrahedron Lett. 28, 2499 (1987); eidem, J. Org. Chem. 53, 1405 (1988). NMR studies: R. J. Cushley et al., Can. J. Chem. 53, 148 (1975). Antimalarial activity: A. J. Castro, Nature 213, 903 (1967). Review: R. P. Williams, W. R. Hearn in Antibiotics vol. 2, D. Gottlieb, P. D. Shaw, Eds. (Springer-Verlag, New York, 1967) pp 410-432, 449-451. Review of synthesis: A. H. Jackson, K. M. Smith, in The Total Synthesis of Natural Products vol. 1, J. ApSimon, Ed. (Wiley-Interscience, New York, 1973) pp 227-232; of biological activity and production: V. Alonzo, Ig. Mod. 81, 557-564 (1984), C.A. 101, 126398h (1984).