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

Gusperimus CAS Registry Number: 104317-84-2 胍立莫司

CAS Name: 7-[(Aminoiminomethyl)amino]-N-[2-[[4-[(3-aminopropyl)amino]butyl]amino]-1-hydroxy-2-oxoethyl]heptanamide
Additional Names: (±)-N-[[[4-[(3-aminopropyl)amino]butyl]carbamoyl]hydrox...
Literature References: Synthetic derivative of the antitumor antibiotic spergualin. Prepn: BE 894651; H. Umezawa et al., US 4518532 (1983, 1985 both to Microbiochem. Res. Found.); Y. Umeda et al., J. Antibiot. 38, 886 (1985). Prepn of the active (-)-isomer: H. Iwasawa et al., ibid. 35, 1665 (1982); H. Umezawa et al., EP 94632; eidem, US 4525299 (1983, 1985 both to Microbiochem. Res. Found.). Synthesis and bioactivity of isomers: Y. Umeda et al., J. Antibiot. 40, 1316 (1987). Mechanism of action study: W. E. G. Müller et al., ibid. 1028. HPLC determn in plasma: R. Nakanuma et al., J. Chromatogr. 527, 208 (1990). Pharmacokinetics: J. F. Muindi et al., Cancer Res. 51, 3096 (1991). Preliminary evaluation in renal transplant rejection: H. Amemiya et al., Transplant. Proc. 25, 730 (1993). Series of articles on synthesis and immunomodulating activity: Ann. N.Y. Acad. Sci. 685, 123-206 (1993).

Dromostanolone CAS Registry Number: 58-19-5 屈他雄酮

CAS Name: (2a,5a,17b)-17-Hydroxy-2-methyl-androstan-3-one
Additional Names: 17b-hydroxy-2a-methyl-5a-androstan-3-one; 2a-methylandrostan-17b-ol-3-one; 2a-methyldihydrotestosterone; drostanolone...
Literature References: Synthetic estrogen antagonist. Prepn: H. J. Ringold et al., J. Am. Chem. Soc. 81, 427 (1959); H. J. Ringold, G. Rosenkranz, US 3118915 (1964 to Syntex). GC-MS determn of urinary metabolites: D. DeBoer et al., J. Steroid Biochem. Mol. Biol. 42, 411 (1992).

AMPA CAS Registry Number: 77521-29-0 (R,S)-Α-氨基-3-羟基-5-甲基-4-异恶唑丙酸

CAS Name: a-Amino-2,3-dihydro-5-methyl-3-oxo-4-isoxazolepropanoic acid
Additional Names: a-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid
Percent Composition: C 45.16%, H 5.41%, N 15.05%...
Literature References: Synthetic excitatory amino acid that characterizes a specific subset of ionotropic glutamate receptors in the CNS, consequently known as AMPA-receptors. The activity resides primarily in the L-isomer. Prepn: J. J. Hansen, P. Krogsgaard-Larsen, J. Chem. Soc. Perkin Trans. 1 1980, 1826; M. Begtrup, F. A. Slok, Synthesis 1993, 861. Characterization of neuroexcitatory activity: P. Krogsgaard-Larsen et al., Nature 284, 64 (1980). Resolution of enantiomers and stereospecific activity: J. J. Hansen et al., J. Med. Chem. 26, 901 (1983). Review of AMPA receptors: K. Borges, R. Dingledine, Prog. Brain Res. 116, 153-170 (1998); and potential for pharmacological intervention: G. J. Lees, Drugs 59, 33-78 (2000).

Vinconate CAS Registry Number: 70704-03-9 长春考酯

CAS Name: 3-Ethyl-2,3,3a,4-tetrahydro-1H-indolo[3,2,1-de][1,5]naphthyridine-6-carboxylic acid methyl ester
Additional Names: chanodesethylapovincamine
Percent Composition: C 72.95%, H 6.80%,...
Literature References: Synthetic hexahydrocanthane alkaloid; vincamine analog. Prepn: BE 870887; J. A. A. Hannart, US 4200638 (1979, 1980 both to Omnium Chim.). Pharmacology: K. Ninomiya et al., Iyakuhin Kenkyu 23, 620 (1992), C.A. 118, 32823 (1992). Pharmacokinetics: M. Kinbara, Y. Satou, ibid. 275, C.A. 117, 123938 (1992). Nootropic activity: H. Kinoshita et al., Res. Commun. Chem. Pathol. Pharmacol. 84, 175 (1994). Clinical pharmacology: B. Saletu et al., Arch. Gerontol. Geriatr. 3, 127 (1984). Acute toxicity study: N. Nishimura et al., Yakuri to Chiryo 20, Suppl. 8, S1995 (1992), C.A. 118, 52241 (1992).

Fluvastatin CAS Registry Number: 93957-54-1 氟伐他汀

CAS Name: (3R,5S,6E)-rel-7-[3-(4-Fluorophenyl)-1-(1-methylethyl)-1H-indol-2-yl]-3,5-dihydroxy-6-heptenoic acid
Additional Names: (±)-(3R*,5S*,6E)-7-[3-(p-fluorophenyl)-1-isopropylindol-2-y...
Literature References: Synthetic HMG-CoA reductase inhibitor. Prepn: F. G. Kathawala, WO 8402131; idem, US 4739073 (1984, 1988 both to Sandoz). Clinical pharmacology: J. Yuan et al., Atherosclerosis 87, 147 (1991). Clinical pharmacokinetics: F. L. S. Tse et al., J. Clin. Pharmacol. 32, 630 (1992). Metabolism in humans: J. G. Dain et al., Drug Metab. Dispos. 21, 567 (1993). HPLC determn in plasma: G. Kalafsky et al., J. Chromatogr. 614, 307 (1993). Clinical study in familial hypercholesterolaemia: E. Leitersdorf et al., Eur. J. Clin. Pharmacol. 45, 513 (1993); in prevention of cardiac events following percutaneous coronary intervention: P. W. J. Serruys et al., J. Am. Med. Assoc. 287, 3215 (2002). Review of pharmacology and therapeutic use: R. I. Levy et al., Circulation 87, Suppl. III, III-45-III-53 (1993).

Cinnamyl Anthranilate CAS Registry Number: 87-29-6 邻氨基苯甲酸肉桂酯

CAS Name: 2-Aminobenzoic acid 3-phenyl-2-propenyl ester
Additional Names: anthranilic acid cinnamyl ester; 3-phenyl-2-propenyl anthranilate; cinnamyl o-aminobenzoate
Percent Composition: C 7...
Literature References: Synthetic imitation grape or cherry flavoring agent. Prepn: A. Seldner, Am. Perfum. Essent. Oil Rev. 54, 295 (1949); R. P. Staiger, E. B. Miller, J. Org. Chem. 24, 1214 (1959). Carcinogenicity studies: G. D. Stoner et al., Cancer Res. 33, 3069 (1973); Fed. Regist. 45, 85832 (1980). Review: D. L. Opdyke, Food Cosmet. Toxicol. 13, Suppl., 751-752 (1975).

Batimastat CAS Registry Number: 130370-60-4 巴马司他

CAS Name: (2R,3S)-N4-Hydroxy-N1-[(1S)-2-(methylamino)-2-oxo-1-(phenylmethyl)ethyl]-2-(2-methylpropyl)-3-[(2-thienylthio)methyl]butanediamide
Additional Names: (2S,3R)-5-methyl-3-[[(aS)-a-(methy...
Literature References: Synthetic matrix metalloproteinase inhibitor. Prepn: C. Campion et al., WO 9005719; eidem, US 5240958 (1990, 1993 both to British Biotech.). Effect on transplanted human ovarian carcinoma: B. Davies et al., Cancer Res. 53, 2087 (1993). Inhibition of metastasis of transplanted human colorectal carcinoma: X. Wang et al., ibid. 54, 4726 (1994).

Motexafin Lutetium CAS Registry Number: 246252-04-0; 156436-90-7 (hydrate)

CAS Name: (PB-7-11-233'2'4)-Bis(acetato-kO)[9,10-diethyl-20,21-bis[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]-4,15-dimethyl-8,11-imino-3,6:16,13-dinitrilo-1,18-benzodiazacycloeicosine-5,14-dipropanolato...
Literature References: Synthetic metal-coordinating expanded porphyrin. Diamagnetic photosensitizer that is activated using far-red light to generate cytotoxic singlet oxygen. Prepn: J. L. Sessler et al., US 5801229 (1998 to Board of Regents Univ. of Texas); S. W. Young et al., Photochem. Photobiol. 63, 892 (1996). Electrochemical characteristics: J. L. Sessler et al., J. Alloys Compds. 249, 146 (1997); and singlet oxygen generation: L. I. Grossweiner et al., Photochem. Photobiol. 70, 138 (1999). LC-MS/MS and ICP-AES determn in plasma: D. Miles et al., AAPS PharmSci. 5, 1 (2003). Preclinical studies in cancer and atheromatous plaque: K. W. Woodburn et al., J. Clin. Laser Med. Surg. 14, 343 (1996); in ocular angiography: M. S. Blumenkranz et al., Am. J. Ophthalmol. 129, 353 (2000). Clinical evaluation in coronary arterial photodynamic therapy: D. J. Kereiakes et al., Circulation 108, 1310 (2003). Review of chemistry and therapeutic potential: T. D. Mody, J. L. Sessler, J. Porphr. Phthalocyan. 5, 134-142 (2001).

Motexafin Gadolinium CAS Registry Number: 246252-06-2; 156436-89-4 (hydrate)

CAS Name: (PB-7-11-233'2'4)-Bis(acetato-kO)[9,10-diethyl-20,21-bis[2-[2-(2-methoxyethoxy)ethoxy]ethoxy]-4,15-dimethyl-8,11-imino-3,6:16,13-dinitrilo-1,18-benzodiazacycloeicosine-5,14-dipropanolato...
Literature References: Synthetic metal-coordinating expanded porphyrin. Paramagnetic redox mediator and radiation enhancer. Prepn: J. L. Sessler et al., US 5801229 (1998 to Board of Regents Univ. of Texas); and redox chemistry: J. L. Sessler et al., J. Phys. Chem. A 103, 787 (1999). Tumor selective radiosensitizing activity and MRI characteristics: S. W. Young et al., Proc. Natl. Acad. Sci. USA 93, 6610 (1996). HPLC determn in plasma: R. A. Parise et al., J. Chromatogr. B 749, 145 (2000). Mechanism of action study: D. Magda et al., Int. J. Radiat. Oncol. Biol. Phys. 51, 1025 (2001); S. I. Hashemy et al., J. Biol. Chem. 281, 10691 (2006). Clinical pharmacokinetics: D. I. Rosenthal et al., Clin. Cancer Res. 5, 739 (1999). Clinical evaluation with radiation in brain metastases: M. P. Mehta et al., J. Clin. Oncol. 20, 3445 (2002); C. A. Meyers et al., J. Clin. Oncol. 22, 157 (2004). Review of chemistry: T. D. Mody, J. L. Sessler, J. Porphyr. Phthalocyan. 5, 134-142 (2001); of therapeutic potential in brain tumors: D. Khuntia, M. Mehta, Expert Rev. Anticancer Ther. 4, 981-989 (2004).

Carumonam CAS Registry Number: 87638-04-8 卡芦莫南

CAS Name: [[(Z)-[2-[[(2S,3S)-2-[[(Aminocarbonyl)oxy]methyl]-4-oxo-1-sulfo-3-azetidinyl]amino]-1-(2-amino-4-thiazolyl)-2-oxoethylidene]amino]oxy]acetic acid
Additional Names: (Z)-[[[(2-amino-4-t...
Literature References: Synthetic monocyclic b-lactam (monobactam) antibiotic. Prepn: S. Kishimoto et al., EP 93376; T. Matsuo et al., US 4572801 (1983, 1986 both to Takeda); M. Sendai et al., J. Antibiot. 38, 346 (1985). Alternate synthesis: P. S. Manchard et al., J. Org. Chem. 53, 5507 (1988). Comparative in vitro antimicrobial activity: R. J. Fass, V. L. Helsel, Antimicrob. Agents Chemother. 28, 834 (1985); B. R. Smith et al., ibid. 29, 346 (1986); I. M. Hoepelman et al., Chemotherapy (Basel) 33, 103 (1987). b-Lactamase stability: R. L. Then, ibid. 30, 398 (1984). Pharmacokinetics in humans: E. Weidekamm et al., Antimicrob. Agents Chemother. 26, 898 (1984); C. A. M. McNulty et al., ibid. 28, 425 (1985).