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

Rosaramicin CAS Registry Number: 35834-26-5 蔷薇霉素

CAS Name: 4'-Deoxycirramycin A1
Additional Names: 3-ethyl-7-hydroxy-2,8,12,16-tetramethyl-5,13-dioxo-9-[[3,4,6-trideoxy-3-(dimethylamino)-b-D-xylo-hexopyranosyl]oxy]-4,17-dioxabicyclo[14.1.0]he...
Literature References: Macrolide antibiotic isolated from fermentations of Micromonospora rosaria NRRL-3718. Isoln and properties: M. J. Weinstein et al., ZA 7100402; FR 2081448 (1971, 1972 both to Sherico), C.A. 76, 139065n (1972); 78, 109310n (1973); G. H. Wagman et al., J. Antibiot. 25, 641 (1972). Biological studies: J. A. Waitz et al., ibid. 647. Structure: H. Reimann, R. S. Jaret, Chem. Commun. 1972, 1270. Crystal structure: A. K. Ganguly et al., Tetrahedron Lett. 21, 4699 (1980). Biosynthesis: A. K. Ganguly et al., J. Antibiot. 29, 976 (1976). Identity with juvenimicin A3: T. Kishi et al., ibid. 1171. Isoln from M. capillata MCRL 0940 and identity with antibiotic M-4365A2: A. Kinumaki et al., ibid. 30, 450 (1977). In vitro activity: S. Feltham et al., J. Antimicrob. Chemother. 5, 731 (1979). Use in experimental pneumococcal meningitis: C. M. Nolan et al., Antimicrob. Agents Chemother. 16, 776 (1979).

Josamycin CAS Registry Number: 16846-24-5 交沙霉素

CAS Name: Leucomycin V 3-acetate 4B-(3-methylbutanoate)
Additional Names: leucomycin A3Trademarks: Iosalide (Schering); Jomybel (Sarva); Josamina (Novag)
Percent Composition: C 60.92%, H 8.4...
Literature References: Macrolide antibiotic produced by Streptomyces narbonensis var. josamyceticus nov. var. Isoln and characterization: T. Osono et al., J. Antibiot. 20A, 174 (1967). Manuf process: H. Umezawa,T. Osono, JP 66 21759 (1966 to Microbiochemical Res. Found.), C.A. 66, 54258w (1967). Prepn: Y. Oka et al., JP Kokai 76 41497 (1976 to Yamanouchi), C.A. 85, 121788b (1976). Identification with leucomycin A3: S. Omura et al., J. Antibiot. 23, 511 (1970). Structure: eidem, ibid. 27, 366 (1974). Absolute configuration: A. Ducruix et al., Chem. Commun. 1976, 947. Stereospecific total synthesis: K. Tatsuta et al., Tetrahedron Lett. 1980, 2837. Retrosynthetic studies: K. C. Nicolaou et al., J. Am. Chem. Soc. 103, 1222 (1981). A 17-membered aglycone was proposed at one time, see T. Osono, H. Umezawa in Drug Action and Drug Resistance in Bacteria 1, S. Mitsuhashi, Ed. (University Park Press, Baltimore, 1971) pp 41-120; T. Osono et al., J. Antibiot. 27, 366 (1974). Pharmacology: K. Kuriaki et al., Jpn. J. Antibiot. 22, 232 (1969). Review: T. Osono, H. Umezawa, loc. cit.

Lankamycin CAS Registry Number: 30042-37-6 久慈霉素B

Additional Names: Kujimycin B
Percent Composition: C 60.56%, H 8.71%, O 30.73%
Literature References: Macrolide antibiotic produced by Streptomyces violaceoniger from soil of Ceylon. Isolation: Gaumann et al., Helv. Chim. Acta 43, 601 (1960). Yields on hydrolysis an aglucone, monoacetyllankolid, C26H48O10, and two sugar-like substances, lankavose (D-chalcose, q.v.) and acetylarcanose: Keller-Schierlein, Roncari, ibid. 45, 138 (1962). Structure: eidem, ibid. 47, 78 (1964); Egan, Martin, J. Am. Chem. Soc. 92, 4129 (1970). Stereochemistry: Muntwyler, Keller-Schierlein, Helv. Chim. Acta 55, 460 (1972). Identity with kujimycin B: Omura et al., J. Antibiot. 22, 629 (1969).

Miokamycin CAS Registry Number: 55881-07-7 醋酸麦迪霉素

CAS Name: Leucomycin V 3B,9-diacetate 3,4B-dipropanoate
Additional Names: 9,3''-diacetylmidecamycin; MOM; ponsinomycin
Trademarks: Miocamycin (Meiji)
Percent Composition: C 60.18%, H 7.97...
Literature References: Macrolide antibiotic; deriv of midecamycin A1. Prepn: S. Inoue et al., JP Kokai 74 124087; eidem, US 4017607 (1974, 1977 both to Meiji Seika); S. Omoto et al., J. Antibiot. 29, 536 (1976); T. Nakamura et al., Chem. Lett. 1978, 1293. Prepn of noncrystalline form and comparison of physico-pharmaceutical properties: T. Sato et al., Chem. Pharm. Bull. 29, 2675 (1981). Antibacterial spectrum: K. Kawaharajo et al., J. Antibiot. 34, 436 (1981). Metabolism: T. Shomura et al., Chem. Pharm. Bull. 29, 2413 (1981). Laboratory and clinical pediatric studies: Y. Toyonaga et al., Jpn. J. Antibiot. 35, 1475 (1982), C.A. 98, 216y (1983). Clinical bioavailability: F. Fraschini et al., Int. J. Clin. Pharmacol. Res. 10, 293 (1989).

Tilmicosin CAS Registry Number: 108050-54-0 替米考星

CAS Name: 4A-O-De(2,6-dideoxy-3-C-methyl-a-L-ribo-hexopyranosyl)-20-deoxo-20-(3,5-dimethyl-1-piperidinyl)tylosin
Additional Names: 20-deoxo-20-(3,5-dimethylpiperidin-1-yl)desmycosinTrademarks: ...
Literature References: Macrolide antibiotic; structurally related to tylosin, q.v. Prepd as 85:15 mixture of cis/trans isomers: M. Debono, H. A. Kirst, EP 103465; eidem, US 4820695 (1984, 1989 both to Lilly); M. Debono et al., J. Antibiot. 42, 1253 (1989). In vitro antibacterial activity: E. E. Ose, ibid. 40, 190 (1987). Metabolism and tissue residue studies in cattle: A. L. Donoho et al., ACS Symp. Ser. 503, 158-167 (1992). Trial in treatment of calf pneumonia: E. E. Ose, L. V. Tonkinson, Vet. Rec. 123, 367 (1988). Prophylactic efficacy in bovine respiratory tract disease: D. W. Morck et al., J. Am. Vet. Med. Assoc. 202, 273 (1993).

Tacrolimus CAS Registry Number: 104987-11-3 他克莫司

CAS Name: (3S,4R,5S,8R,9E,12S,14S,15R,16S,18R,19R,26aS)-5,6,8,11,12,13,14,15,16,17,18,19,24,25,26,26a-Hexadecahydro-5,19-dihydroxy-3-[(1E)-2-[(1R,3R,4R)-4-hydroxy-3-methoxycyclohexyl]-1-methylethe...
Literature References: Macrolide isolated from Streptomyces tsukubaensis no. 9993: M. Okuhara et al., EP 184162 (1986 to Fujisawa); and characterization: T. Kino et al., J. Antibiot. 40, 1249 (1987). Structure determn: H. Tanaka et al., J. Am. Chem. Soc. 109, 5031 (1987). Total synthesis of (-)-form: T. K. Jones et al., J. Am. Chem. Soc. 111, 1157 (1989). In vitro immunosuppressant activity in comparison with cyclosporin, q.v.: T. Kino et al., J. Antibiot. 40, 1256 (1987). Toxicology: K. Ohara et al., Transplant. Proc. 22, 83 (1990). Symposium on pharmacology and clinical trials: ibid. 23, 2709-3376 (1991). Review of mechanism of action: G. Wiederrecht et al., Ann. N.Y. Acad. Sci. 696, 9-19 (1993); of clinical trials in comparison with cyclosporin in renal transplantation: G. A. Knoll, R. C. Bell, Br. Med. J. 318, 1104-1107 (1999). Review of use in dermatoses: A. K. Gupta et al., J. Eur. Acad. Dermatol. Venereol. 16, 100-114 (2002).

Nonactin CAS Registry Number: 6833-84-7 无活菌素来源于灰色链霉菌变种

CAS Name: (1R,2R,5R,7R,10S,11S,14S,16S,19R,20R,23R,25R,28S,29S,32S,34S)-2,5,11,14,20,23,29,32-Octamethyl-4,13,22,31,37,38,39,40-octaoxapentacyclo-[32.2.1.17,10.116,19.125,28]tetracontane-3,12,21,3...
Literature References: Macrotetrolide antibiotic. Produced by several Streptomyces spp.: Corbaz et al., Helv. Chim. Acta 38, 1445 (1955); Wallhäusser et al., Arzneim.-Forsch. 14, 356 (1964). Structure: Dominguez et al., Helv. Chim. Acta 45, 129 (1962). Crystal structure: Dobler, ibid. 55, 1371 (1972). Steroselective syntheses of nonactic acid, building block of nonactin: Gerlach, Wetter, ibid. 57, 2306 (1974); R. E. Ireland, J.-P. Vevert, J. Org. Chem. 45, 4260 (1980). Total synthesis of (+)- and (-)-nonactic acids: eidem, Can. J. Chem. 59, 572 (1981). Synthesis of nonactin: Gombos et al., Monatsh. Chem. 106, 1043 (1975); eidem, Tetrahedron Lett. 1975, 3391; Gerlach et al., Helv. Chim. Acta 58, 2036 (1975); U. Schmidt et al., Ber. 109, 2628 (1976). Three homologs, monactin, C41H66O12, dinactin, C42H68O12, and trinactin, C43H70O12 are known: Beck et al., Helv. Chim. Acta 45, 620 (1962); Gerlach, Prelog, Ann. 669, 121 (1963). Activity of nonactin and its homologues: Meyers et al., J. Antibiot. 18A, 128 (1965). Biosynthesis study: J. E. Cox, N. D. Priestley, J. Am. Chem. Soc. 127, 7976 (2005).

Chloral Hydrate CAS Registry Number: 302-17-0 水合氯醛

CAS Name: 2,2,2-Trichloro-1,1-ethanediol
Additional Names: trichloroacetaldehyde monohydrate
Trademarks: Escre (SS Pharm.); Noctec (BMS); Nycton; Somnos (Merck Co.); Chloraldurat (Pohl)
...
Literature References: Made by adding the required amount of water to trichloroacetaldehyde, q.v. First synthesized by Liebig in 1832. Introduced as hypnotic by Liebreich in 1869. Comprehensive description: J. E. Fairbrother, Anal. Profiles Drug Subs. 2, 85-143 (1973). Toxicity data: E. Goldenthal, Toxicol. Appl. Pharmacol. 18, 185 (1971). Evaluation of mutagenicity: J. Leuschner, F. Leuschner, Arzneim.-Forsch. 41, 1101 (1991).

o-Tolidine CAS Registry Number: 119-93-7 3,3'-二甲基联苯胺

CAS Name: 3,3'-Dimethyl-[1,1'-biphenyl]-4,4'-diamine
Additional Names: 3,3'-dimethylbenzidine; 4,4'-diamino-3,3'-dimethylbiphenyl
Percent Composition: C 79.21%, H 7.60%, N 13.20%
Literature References: Made by alkaline reduction of o-nitrotoluene with zinc, and subsequent rearrangement of the o-hydrazotoluene formed, by boiling with HCl: Van Loon, Chem. Weekbl. 5, 689 (1907). See also Schultz et al., Ann. 352, 111 (1907). Crystal and molecular structure: Chawdhury et al., Acta Crystallogr. B24, 1222 (1968). Metabolism: Dieteren, Arch. Environ. Health 12, 30 (1966). Carcinogenic activity: Pliss, Zebenzhinskii, J. Natl. Cancer Inst. 45, 283 (1970).

Diazoaminobenzene CAS Registry Number: 136-35-6 苯氨基重氮苯

CAS Name: 1,3-Diphenyl-1-triazene
Additional Names: anilinoazobenzene; benzeneazoaniline
Percent Composition: C 73.07%, H 5.62%, N 21.30%
Literature References: Made by diazotizing aniline dissolved in HCl with NaNO2 and then adding a concd soln of sodium acetate: Hartman, Dickey, Org. Synth. coll. vol. II, 163 (1943).