HRID412991

反应详情

EQUATION

反应方程式

REACTANTS

反应物

HCID65432

1,4-Dioxane-2,5-dione

C4H4O4

HCID178435178

未命名化合物

结构：CC(=O)O.CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1

HCID178476396

未命名化合物

PRODUCTS

生成物

结构：CCNC(=O)[C@@H]1CCCN1C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@H](CC(C)C)NC(=O)[C@@H](CC(C)C)NC(=O)[C@H](Cc1ccc(O)cc1)NC(=O)[C@H](CO)NC(=O)[C@H](Cc1c[nH]c2ccccc12)NC(=O)[C@H](Cc1c[nH]cn1)NC(=O)[C@@H]1CCC(=O)N1

HCID178465153

未命名化合物

AUXILIARIES

试剂、催化剂与溶剂

溶剂HCID962

Water

H2O

溶剂HCID13387

N-Methyl-2-pyrrolidone

C5H9NO

PROCEDURE

实验过程

Poly(DL-lactide-co-glycolide) with a molar ratio of lactide to glycolide of 75/25 (Birmingham Polymer, Inc.) was dissolved in NMP to give a solution with 45% by weight polymer. This solution was filled into 3.0 cc polyproylene syringes with a male luer lock fitting and terminally sterilized by exposure to gamma irradiation at 23.2-24.6 kilograys. The polymer molecular weight after irradiation was 15,094 daltons. Leuprolide acetate was dissolved in water, sterile filtered through 0.2 mm filter and filled into a polypropylene syringe with a male luer lock fitting. The aqueous solution was frozen and the water removed by vacuum to yield a lyophilized cake of leuprolide. The two syringes were connected together with a coupler immediately prior to use and the contents of the two syringes mixed by moving the material back and forth between the two syringes for 40 cycles to provide a formulation with 6% by weight of leuprolide acetate. The product was then pulled into the syringe with the male luer lock fitting one a one-half inch 20 gauge needle attached.

WORKUP

后处理

customto give a solution with 45% by weight polymer
customterminally sterilized by exposure to gamma irradiation at 23.2-24.6 kilograys
customThe polymer molecular weight after irradiation
filtrationsterile filtered through 0.2 mm
filtrationfilter
additionfilled into a polypropylene syringe with a male luer lock
temperatureThe aqueous solution was frozen
customthe water removed by vacuum

来源与证据

来源类型: Open Reaction Database
ORD 记录: ord-99951c4a067a46c7b16d996c7f586156
来源数据集: uspto-grants-2003_05
DOI: 10.6084/m9.figshare.5104873.v1
专利: US06565874B1
来源说明: uspto-grants-2003_05

反应 SMILES

C1OC(=O)COC1=O.[CH3:9][CH2:10][NH:11][C:12]([C@H:14]1[N:18]([C:19]([C@@H:21]([NH:29][C:30]([C@@H:32]([NH:37][C:38]([C@H:40]([NH:45][C:46]([C@@H:48]([NH:57][C:58]([C@@H:60]([NH:63][C:64]([C@@H:66]([NH:77][C:78]([C@@H:80]([NH:87][C:88]([C@H:90]2[NH:95][C:93](=[O:94])[CH2:92][CH2:91]2)=[O:89])[CH2:81][C:82]2[N:86]=[CH:85][NH:84][CH:83]=2)=[O:79])[CH2:67][C:68]2[C:72]3[CH:73]=[CH:74][CH:75]=[CH:76][C:71]=3[NH:70][CH:69]=2)=[O:65])[CH2:61][OH:62])=[O:59])[CH2:49][C:50]2[CH:51]=[CH:52][C:53]([OH:56])=[CH:54][CH:55]=2)=[O:47])[CH2:41][CH:42]([CH3:44])[CH3:43])=[O:39])[CH2:33][CH:34]([CH3:36])[CH3:35])=[O:31])[CH2:22][CH2:23][CH2:24][NH:25][C:26]([NH2:28])=[NH:27])=[O:20])[CH2:17][CH2:16][CH2:15]1)=[O:13].CC(O)=O>CN1C(=O)CCC1.O>[CH3:9][CH2:10][NH:11][C:12]([C@H:14]1[N:18]([C:19]([C@@H:21]([NH:29][C:30]([C@@H:32]([NH:37][C:38]([C@H:40]([NH:45][C:46]([C@@H:48]([NH:57][C:58]([C@@H:60]([NH:63][C:64]([C@@H:66]([NH:77][C:78]([C@@H:80]([NH:87][C:88]([C@H:90]2[NH:95][C:93](=[O:94])[CH2:92][CH2:91]2)=[O:89])[CH2:81][C:82]2[N:86]=[CH:85][NH:84][CH:83]=2)=[O:79])[CH2:67][C:68]2[C:72]3[CH:73]=[CH:74][CH:75]=[CH:76][C:71]=3[NH:70][CH:69]=2)=[O:65])[CH2:61][OH:62])=[O:59])[CH2:49][C:50]2[CH:55]=[CH:54][C:53]([OH:56])=[CH:52][CH:51]=2)=[O:47])[CH2:41][CH:42]([CH3:44])[CH3:43])=[O:39])[CH2:33][CH:34]([CH3:36])[CH3:35])=[O:31])[CH2:22][CH2:23][CH2:24][NH:25][C:26]([NH2:28])=[NH:27])=[O:20])[CH2:17][CH2:16][CH2:15]1)=[O:13]