制备方法

环丝氨酸可用发酵法或直接合成法制备。发酵法产生菌是赖氏放线菌(Actinomyces laven-dulae),发酵培养基为糊精、葡萄糖、淀粉、黄豆饼粉、酵母粉、硫酸铵、硝酸铵、碳酸钙、氯化钠、硫酸镁和豆油等。合成法是将β-氨基氧丙氨酸乙酯二盐酸盐和氢氧化钾反应,即环合得到环丝氨酸。

合成制备方法

环丝氨酸可用发酵法或直接合成法制备。发酵法产生菌是赖氏放线菌（Actinomyces laven-dulae），发酵培养基为糊精、葡萄糖、淀粉、黄豆饼粉、酵母粉、硫酸铵、硝酸铵、碳酸钙、氯化钠、硫酸镁和豆油等。合成法是将β-氨基氧丙氨酸乙酯二盐酸盐和氢氧化钾反应，即环合得到环丝氨酸。

用途简介

抗菌素类药。用于耐药性结核杆菌的感染。

用途

抗菌素类药。用于耐药性结核杆菌的感染。

海关代码：

2934999090

危险类别码：

R5

安全说明：

S24/25

安全标志：

S38:在通风不良的场所，佩戴合适的呼吸装置。
S24/25:防止皮肤和眼睛接触。
:

危险标志：

Xn

CHEMICAL IDENTIFICATION

RTECS NUMBER :

NY2975000

CHEMICAL NAME :

3-Isoxazolidinone, 4-amino-, D-

CAS REGISTRY NUMBER :

68-41-7

BEILSTEIN REFERENCE NO. :

0080798

LAST UPDATED :

199612

DATA ITEMS CITED :

20

MOLECULAR FORMULA :

C3-H6-N2-O2

MOLECULAR WEIGHT :

102.11

WISWESSER LINE NOTATION :

T5OMVTJ DZ -D

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human

DOSE/DURATION :

560 mg/kg/4W-I

TOXIC EFFECTS :

Behavioral - wakefulness Behavioral - tremor

REFERENCE :

DICHAK Diseases of the Chest. (Chicago, IL) V.1-56, 1935-69. For publisher information, see CHETBF. Volume(issue)/page/year: 29,241,1956

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

60 mg/kg

TOXIC EFFECTS :

Behavioral - coma

REFERENCE :

BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 1,907,1965

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Unreported

SPECIES OBSERVED :

Human - woman

DOSE/DURATION :

40 mg/kg/2D-I

TOXIC EFFECTS :

Behavioral - hallucinations, distorted perceptions

REFERENCE :

TUBEAS Tubercle. (Williams & Wilkins Co., 428 E. Preston Street, Baltimore, MD 21202) V.1- 1919- Volume(issue)/page/year: 38,297,1957

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Unreported

SPECIES OBSERVED :

Human - man

DOSE/DURATION :

64 mg/kg/4D-I

TOXIC EFFECTS :

Behavioral - sleep Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold

REFERENCE :

ABANAE Antibiotics Annual. (New York, NY) 1953-60. For publisher information, see AMACCQ. Volume(issue)/page/year: 3,148,1955/1956

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>5 gm/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity)

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,360,1956

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

>3 gm/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity)

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,360,1956

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

5290 mg/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Behavioral - ataxia

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,360,1956

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

180 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

85FZAT "Index of Antibiotics from Actinomycetes," Umezawa, H. et al., eds., Tokyo, Univ. of Tokyo Press, 1967 Volume(issue)/page/year: -,238,1967

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

1400 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 31,1085,1980

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

560 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 31,1085,1980

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

>2 gm/kg

TOXIC EFFECTS :

Gastrointestinal - nausea or vomiting

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,360,1956

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

2 gm/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Behavioral - tremor Gastrointestinal - nausea or vomiting

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,708,1956

TYPE OF TEST :

LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Primate - monkey

DOSE/DURATION :

4 gm/kg

TOXIC EFFECTS :

Behavioral - somnolence (general depressed activity) Behavioral - ataxia Gastrointestinal - nausea or vomiting

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,708,1956

TYPE OF TEST :

LD - Lethal dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - rabbit

DOSE/DURATION :

>2 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,382,1956

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - guinea pig

DOSE/DURATION :

>2 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,360,1956

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Rodent - guinea pig

DOSE/DURATION :

>1 gm/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,360,1956 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Subcutaneous

SPECIES OBSERVED :

Mammal - dog

DOSE/DURATION :

15 gm/kg/60D-I

TOXIC EFFECTS :

Blood - pigmented or nucleated red blood cells Blood - changes in erythrocyte (RBC) count Related to Chronic Data - death

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,708,1956

TYPE OF TEST :

TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Primate - monkey

DOSE/DURATION :

45 gm/kg/90D-I

TOXIC EFFECTS :

Gastrointestinal - hypermotility, diarrhea Blood - changes in bone marrow (not otherwise specified) Related to Chronic Data - death

REFERENCE :

ANTCAO Antibiotics and Chemotherapy (Washington, DC). (Washington, DC) V.1-12, 1951-62. For publisher information, see CLMEA3. Volume(issue)/page/year: 6,708,1956 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5527 No. of Facilities: 31 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 756 (estimated) No. of Female Employees: 559 (estimated)

中国海关编码：2934999090

概述：

2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

申报要素：

品名, 成分含量, 用途

摘要/Summary：

2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

分子结构数据

1、  摩尔折射率：22.47

2、  摩尔体积（cm³/mol）：79.8

3、  等张比容（90.2K）：201.9

4、  表面张力（dyne/cm）：40.8

5、  极化率（10-24cm3）：8.90

 

计算化学数据

1、   疏水参数计算参考值（XlogP）：-1.5

2、   氢键供体数量：2

3、   氢键受体数量：3

4、   可旋转化学键数量：0

5、   互变异构体数量：5

6、   拓扑分子极性表面积（TPSA）：64.4

7、   重原子数量：7

8、   表面电荷：0

9、   复杂度：92.9

10、   同位素原子数量：0

11、   确定原子立构中心数量：1

12、   不确定原子立构中心数量：0

13、   确定化学键立构中心数量：0

14、   不确定化学键立构中心数量：0

15、   共价键单元数量：1

• 
  D-环丝氨酸红外图谱(IR1)
• 
  D-环丝氨酸红外图谱(IR2)
• 
  D-环丝氨酸质谱(MS)
• 
  D-环丝氨酸核磁图(¹³CNMR)
• 
  D-环丝氨酸核磁图(¹HNMR)