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

Amylpenicillin CAS Registry Number: 4493-18-9 6a-[(1-氧代己基)氨基]青霉烷酸

CAS Name: (2S,5R,6R)-3,3-Dimethyl-7-oxo-6-[(1-oxohexyl)amino]-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
Additional Names: dihydropenicillin F; hexanoylpenicillin; penicillin DF
Per...
Literature References: Antibiotic produced by the mold Aspergillus flavus from a Czapek-Dox medium supplemented with corn steep liquor or by Penicillium chrysogenum Q176 or by P. notatum strains: McKee, MacPhillamy, Proc. Soc. Exp. Biol. Med. 53, 247 (1943); Bush, Goth, J. Pharmacol. Exp. Ther. 78, 164 (1943); McKee et al., J. Bacteriol. 47, 187 (1944); Bush et al., J. Pharmacol. Exp. Ther. 84, 264 (1945); Fried et al., J. Biol. Chem. 163, 341 (1946); see also Wintersteiner under "Flavacidin" in Chemistry of Penicillin (Princeton, 1949). Prepn by hydrogenation of 2-pentenylpenicillin: Catch et al., GB 584852; Cook, Heilbron in Chemistry of Penicillin (Princeton, 1949). Characterization and antibacterial activity: Leigh, Nature 163, 95 (1949).

Bacilysin CAS Registry Number: 29393-20-2 L-丙氨酸,L-异丙酰-3-[(1R,2S,6R)-5-氧代-7-氧双环[4.1.0]庚-2-基]-

CAS Name: [1R-(1a,2b,6a)]-N-L-Alanyl-3-(5-oxo-7-oxabicyclo[4.1.0]hept-2-yl)-L-alanine
Additional Names: a-[(2-amino-1-oxopropyl)amino]-5-oxo-7-oxabicyclo[4.1.0]heptane-2-propanoic acid; a-(2-am...
Literature References: Antibiotic produced by the soil bacillus NCTC 7197: Gilliver et al., in Antibiotics vol. I, Florey et al., Eds. (Oxford, 1949) p 458. Production by Bacillus subtilis and purification: Rogers et al., Biochem. J. 97, 573 (1965). Identity with tetaine: K. Kaminski, T. Sololowska, J. Antibiot. 26, 184 (1973). Identity with bacillin: K. Atsumi et al., ibid. 28, 77 (1975). Improved isoln: Walker, Abraham, Biochem. J. 118, 557 (1970). Structural study: Rogers et al., ibid. 97, 579 (1965). Final structure: Walker, Abraham, ibid. 118, 563 (1970).

Demeclocycline CAS Registry Number: 127-33-3 地美环素

CAS Name: [4S-(4a,4aa,5aa,6b,12aa)]-7-Chloro-4-(dimethylamino)-1,4,4a,5,5a,6,11,12a-octahydro-3,6,10,12,12a-pentahydroxy-1,11-dioxo-2-naphthacenecarboxamide
Additional Names: 7-chloro-6-demethy...
Literature References: Antibiotic related to tetracycline produced by Streptomyces aureofaciens. Prepn: McCormick et al., J. Am. Chem. Soc. 79, 4561 (1957); US 2878289 (1959 to Am. Cyanamid). Improved fermentation processes: Szumski, US 3012946; Goodman, Matrishin, US 3019172; Goodman, US 3050446 (1961, 1962, 1962 all to Am. Cyanamid); FR 1344645 (1963 to Merck Co.); Neidleman, US 3154476 (1964 to Olin Mathieson). Abs config: Dobrynin et al., Tetrahedron Lett. 1962, 901. Toxicity data: E. I. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971).

Dactinomycin CAS Registry Number: 50-76-0 放线菌素D

CAS Name: Actinomycin D
Additional Names: actinomycin-[thr-val-pro-sar-meval]; meractinomycin; actinomycin AIV; actinomycin IV; actinomycin C1; actinomycin I1; actinomycin X1Trademarks: Cosmege...
Literature References: Antibiotic substance belonging to the actinomycin complex, produced by several Streptomyces spp. Historical background of actinomycins and chemistry, toxicology, pharmacology of actinomycin D: Ann. N.Y. Acad. Sci. 89, 285-485 (1960). Isoln from broth cultures of S. parvulus: Manaker et al., Antibiot. Ann. 1954/55, 853. Structure: Bullock, Johnson, J. Chem. Soc. 1957, 3280. Synthesis: Brockmann, Manegold, Naturwissenschaften 51, 383 (1964); Brockmann, Lackner, ibid. 384, 435 (1964); Brockmann et al., DE 1172680 (1964 to Bayer); eidem, Ber. 101, 1312 (1968); Meienhofer, J. Am. Chem. Soc. 92, 3771 (1970); T. Tanaka et al., Bull. Chem. Soc. Jpn. 53, 1352 (1980); K. Nakajima et al., Pept. Chem. 19, 143-148 (1981). Conformation from NMR: Conti, DeSantis, Nature 227, 1239 (1970); Lackner, Ber. 104, 3653 (1971). Toxicity data: F. S. Philips et al., Ann. N.Y. Acad. Sci. 89, 348 (1960). Review and evaluation of studies of carcinogenic action in laboratory animals: IARC Monographs 12, 29-41 (1976).

Spiramycin CAS Registry Number: 8025-81-8 螺旋霉素

Trademarks: Selectomycin (Grñenthal); Rovamicina (RPR); Rovamycin (RPR)
Literature References: Antibiotic substance classified in the erythromycin-carbomycin group and produced by Streptomyces ambofaciens from soil of northern France: Cosar et al., C.R. Seances Soc. Biol. Ses Fil. 234, 1498 (1952); Pinnert-Sindico et al., Antibiot. Annu. 1954-1955, 724; Ninet, Verrier, US 2943023 (1960 to Rhône-Poulenc), see also US 3000785 (1961 to Rhône-Poulenc). Antibacterial activity and toxicity: H. Sous et al., Arzneim.-Forsch. 8, 386 (1958). Separation into 3 components named spiramycin I, II and III: Preud'homme, Charpentier, US 2978380 and US 3011947 (1961 to Rhône-Poulenc). Structure: Kuehne, Benson, J. Am. Chem. Soc. 87, 4660 (1965). Revised structure: Omura et al., ibid. 91, 3401 (1969); Mitscher et al., J. Antibiot. 26, 55 (1973). Revised configuration at C-9: Freiberg et al., J. Org. Chem. 39, 2474 (1974). Symposium on pharmacology, antibacterial spectrum, and clinical efficacy: J. Antimicrob. Chemother. 22, Suppl. B, 1-213 (1988).

Toyocamycin CAS Registry Number: 606-58-6 丰加霉素

CAS Name: 4-Amino-7-b-D-ribofuranosyl-7H-pyrrolo[2,3-d]pyrimidine-5-carbonitrile
Additional Names: 4-amino-5-cyano-7-(D-ribofuranosyl)-7H-pyrrolo[2,3-d]pyrimidine; uramycin B; vengicide; antibi...
Literature References: Antibiotic substance extracted from the culture filtrate and mycelium of Streptomyces toyocaensis. Isoln: Nishimura et al., J. Antibiot. 9A, 60 (1956). Structure: Ohkuma, ibid. 14A, 343 (1961). Synthesis of aglycone: Taylor, Hendess, J. Am. Chem. Soc. 86, 951 (1964). Total synthesis: Tolman et al., ibid. 90, 524 (1968); 91, 2102 (1969). Biosynthesis: Uematsu, Suhadolnik, Biochemistry 9, 1260 (1970); eidem, J. Biol. Chem. 245, 4365 (1970). Crystal and molecular structure: P. Prusiner, M. Sundaralingam, Acta Crystallogr. B34, 517 (1978).

Mycelianamide CAS Registry Number: 22775-52-6 菌絲醯胺

CAS Name: (6S)-3-[[4-[[(2E)-3,7-Dimethyl-2,6-octadienyl]oxy]phenyl]methylene]-1,4-dihydroxy-6-methyl-2,5-piperazinedione
Percent Composition: C 65.98%, H 7.05%, N 7.00%, O 19.98%
Literature References: Antibiotic substance found in the mycelium of Penicillium griseofulvum: Anslow, Raistrick, Biochem. J. 25, 39 (1931); Oxford et al., ibid. 29, 1102 (1935); 33, 240 (1939); Oxford, Raistrick, ibid. 42, 323 (1948). Structure: Birch et al., J. Chem. Soc. 1956, 3717; Bates, Schauble, Tetrahedron Lett. 1963, 1683. Configuration: Gallina et al., Gazz. Chim. Ital. 94, 1301 (1964). Partial synthesis: Brown, Meehan, Aust. J. Chem. 21, 1581 (1968). Total synthesis: N. Shinmon et al., Chem. Commun. 1980, 1020.

Viridin CAS Registry Number: 3306-52-3 (1S-(1alpha,2alpha,11balpha))-1,7,8,11b-四氢-1-羟基-2-甲氧基-11b-甲基环戊并(7,8)菲并(10,1-bc)呋喃-3,6,9(2H)-三酮

CAS Name: 1b-Hydroxy-2b-methoxy-18-norandrosta-5,8,11,13-tetraeno[6,5,4-bc]furan-3,7,17-trione
Percent Composition: C 68.18%, H 4.58%, O 27.25%
Literature References: Antibiotic substance from Gliocladium virens: Grove et al., J. Chem. Soc. 1965, 3803. Previously reported isolation from Trichoderma viride: Brian, McGowan, Nature 156, 144 (1945); Brian et al., Ann. Appl. Biol. 33, 190 (1946). Epimerizes to b-viridin where methoxyl group is equatorial. Separation of the two isomers: Vischer et al., Nature 165, 528 (1950). Structure: Grove et al., Chem. Commun. 1965, 343. Configuration: eidem, J. Chem. Soc. C 1966, 743; Neidle, Hursthouse, J. Chem. Soc. Perkin Trans. 2 1972, 760. Biosynthesis: Blight et al., Chem. Commun. 1968, 1117; Grove, J. Chem. Soc. C 1969, 549.

Monorden CAS Registry Number: 12772-57-5 根赤壳菌素

CAS Name: 8-Chloro-1a,14,15,15a-tetrahydro-9,11-dihydroxy-14-methyl-6H-oxireno[e][2]benzoxacyclotetradecin-6,12(7H)-dione
Additional Names: 5-chloro-6-(7,8-epoxy-10-hydroxy-2-oxo-3,5-undecadien...
Literature References: Antibiotic substance from Monosporium bonorden: Delmotte, Delmotte-Plaquée, Nature 171, 344 (1953). Identity with radicicol: Mirrington et al., Tetrahedron Lett. 1964, 365. Structure: McCapra, Scott, ibid. 1964, 869; Mirrington et al., Aust. J. Chem. 19, 1265 (1966). Isoln: NL 6506173 (1965 to Sandoz).

L -Alanosine CAS Registry Number: 5854-93-3 L-丙氨菌素

CAS Name: 3-(Hydroxynitrosoamino)-L-alanine
Additional Names: L-2-amino-3-(hydroxynitrosoamino)propanoic acid; L-2-amino-3-[(N-nitroso)hydroxylamino]propionic acid
Percent Composition: C 24....
Literature References: Antibiotic substance from the fermentation of Streptomyces alanosinicus n. sp. Prepn: NL 6509543; J. Thiemann, Y. S. K. Murthy, US 3676490 (1966, 1972 both to Lepetit). The first natural product found to have a N-nitrosohydroxylamino group on an aliphatic chain. Isoln and structure: Coronelli et al., Farmaco Ed. Sci. 21, 269 (1966). Characterization: Thiemann, Beretta, J. Antibiot. 19A, 155 (1966). Structure and synthesis of L-, D- and DL-forms: Lancini et al., Tetrahedron Lett. 1966, 1769; eidem, Farmaco Ed. Sci. 24, 169 (1969). Synthesis of L-form: Isowa et al., Bull. Chem. Soc. Jpn. 46, 1847 (1973). Improved synthesis of DL-form: Eaton et al., J. Med. Chem. 16, 289 (1973). Pharmacology: Murthy et al., Nature 211, 1198 (1966). Mode of action studies: Gale et al., Biochem. Pharmacol. 17, 363, 1823 (1968). Effect on insect growth: E. E. Kenaga, J. Econ. Entomol. 62, 1006 (1969); S. Matsumoto et al., Agric. Biol. Chem. 48, 827 (1984).