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13127-18-9

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  • Factory Supply (3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-4-((2,6-didesoxy-3-C-methyl-3-O-methyl-α-L-ribo-hexopiranosyl)oxy)-14-ethyl-7,12,13-trihydroxy-3,5,7,9,11,13-hexamethyl-6-((3,4,6-tridesoxy-3-dimeth

    Cas No: 13127-18-9

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13127-18-9 Usage

Chemical Properties

Off-White Solid

Uses

Different sources of media describe the Uses of 13127-18-9 differently. You can refer to the following data:
1. Erythromycin A Oxime (Roxithromycin Impurity C) (Clarithromycin EP Impurity J) is the major metabolite of Roxithromycin and an intermediate of Azithromycin. Antibacterial agent. Roxithromycin impurity C.
2. The major metabolite of Roxithromycin

Check Digit Verification of cas no

The CAS Registry Mumber 13127-18-9 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 1,3,1,2 and 7 respectively; the second part has 2 digits, 1 and 8 respectively.
Calculate Digit Verification of CAS Registry Number 13127-18:
(7*1)+(6*3)+(5*1)+(4*2)+(3*7)+(2*1)+(1*8)=69
69 % 10 = 9
So 13127-18-9 is a valid CAS Registry Number.
InChI:InChI=1/C37H68N2O13/c1-14-25-37(10,45)30(41)20(4)27(38-46)18(2)16-35(8,44)32(52-34-28(40)24(39(11)12)15-19(3)48-34)21(5)29(22(6)33(43)50-25)51-26-17-36(9,47-13)31(42)23(7)49-26/h18-26,28-32,34,40-42,44-46H,14-17H2,1-13H3/b38-27+/t18-,19-,20+,21+,22-,23+,24+,25-,26+,28-,29+,30-,31+,32-,34+,35-,36-,37-/m1/s1

13127-18-9SDS

SAFETY DATA SHEETS

According to Globally Harmonized System of Classification and Labelling of Chemicals (GHS) - Sixth revised edition

Version: 1.0

Creation Date: Aug 13, 2017

Revision Date: Aug 13, 2017

1.Identification

1.1 GHS Product identifier

Product name Erythromycin A Oxime

1.2 Other means of identification

Product number -
Other names ERYTHROMYCIN OXIME

1.3 Recommended use of the chemical and restrictions on use

Identified uses For industry use only.
Uses advised against no data available

1.4 Supplier's details

1.5 Emergency phone number

Emergency phone number -
Service hours Monday to Friday, 9am-5pm (Standard time zone: UTC/GMT +8 hours).

More Details:13127-18-9 SDS

13127-18-9Synthetic route

erythromycin
114-07-8

erythromycin

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

Conditions
ConditionsYield
With hydroxylamine; acetic acid In isopropyl alcohol at 50℃; for 24h;95%
With hydroxylamine hydrochloride; triethylamine In methanol Reflux;93%
With hydroxylamine hydrochloride; potassium carbonate In methanol at 20℃; for 48h; Solvent; Reagent/catalyst; Temperature;88.2%
erythromycin
114-07-8

erythromycin

A

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

B

8,9-anhydropseudoerythromycin A 6,9-hemiketal
105882-69-7

8,9-anhydropseudoerythromycin A 6,9-hemiketal

Conditions
ConditionsYield
With hydroxylamine hydrochloride; sodium acetate In methanol at 50℃; for 13h;
erythromycin A thiocyanate
7704-67-8

erythromycin A thiocyanate

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

Conditions
ConditionsYield
With hydroxylamine hydrochloride In dichloromethane at 20℃; for 1.5h; pH=7; Beckmann Rearrangement;
With hydroxylamine hydrochloride; ammonium bicarbonate; sodium iodide In methanol at 56 - 60℃; Reagent/catalyst;89 g
erythromycin A oxime thiocyanate
1357466-70-6

erythromycin A oxime thiocyanate

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

Conditions
ConditionsYield
With sodium hydroxide In dichloromethane; water at 38℃; Solvent; Temperature;
2-Methoxypropene
116-11-0

2-Methoxypropene

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

1,1,1,3,3,3-hexamethyl-disilazane
999-97-3

1,1,1,3,3,3-hexamethyl-disilazane

C44H84N2O14Si
119685-40-4

C44H84N2O14Si

Conditions
ConditionsYield
Stage #1: 2-Methoxypropene; (9-E)-deoxo-9-hydroximinoerythromycin A With Pyridine hydrobromide In dichloromethane at 7 - 17℃; for 2h;
Stage #2: 1,1,1,3,3,3-hexamethyl-disilazane In dichloromethane for 1h;
Stage #3: With sodium hydrogencarbonate In dichloromethane; water at 27 - 33℃; for 0.5h; Product distribution / selectivity;
96.9%
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

9-deoxo-6-deoxy-6,9-epoxy-9,9a-didehydro-9a-aza-homoerythromycin A
342371-84-0

9-deoxo-6-deoxy-6,9-epoxy-9,9a-didehydro-9a-aza-homoerythromycin A

Conditions
ConditionsYield
With sodium hydrogencarbonate; p-toluenesulfonyl chloride In water; acetone at 0 - 20℃; for 4h;91.8%
With sodium hydrogencarbonate; p-toluenesulfonyl chloride In dichloromethane; water at 0 - 5℃; Product distribution / selectivity;
With sodium hydrogencarbonate; p-toluenesulfonyl chloride In dichloromethane at 20℃; for 1.5h;
With sodium hydrogencarbonate; methanesulfonyl chloride In water at 5℃; Temperature; Reagent/catalyst; Beckmann Rearrangement;
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

erythromycylamine
26116-56-3

erythromycylamine

Conditions
ConditionsYield
With methanol; sodium tetrahydroborate at 20℃; for 8h; Reagent/catalyst; Temperature; Cooling with ice;85.03%
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

9-Deoxo-9a-aza-9a-homoerythromycin A
76801-85-9

9-Deoxo-9a-aza-9a-homoerythromycin A

Conditions
ConditionsYield
Stage #1: (9-E)-deoxo-9-hydroximinoerythromycin A With calcium(II) bis(trifluoromethanesulfonyl)imide; tert-butylammonium hexafluorophosphate(V) In 1,2-dimethoxyethane; 1,2-dichloro-ethane at 80℃; for 5h;
Stage #2: With sodium tetrahydroborate In methanol at 0 - 20℃; for 51h;
78%
Multi-step reaction with 2 steps
1: p-toluenesulfonyl chloride; sodium hydrogencarbonate / acetone; water / 4 h / 0 - 20 °C
2: sodium tetrahydroborate; methanol / 24 h / 0 - 20 °C
View Scheme
1,1-diisopropoxycyclohexane
1132-95-2

1,1-diisopropoxycyclohexane

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

9-{O-[1-(1-methylethoxy)-cyclohexyl]oxime}-erythromycin
129288-91-1

9-{O-[1-(1-methylethoxy)-cyclohexyl]oxime}-erythromycin

Conditions
ConditionsYield
With pyridine hydrochloride In dichloromethane at 20℃; for 42h;71%
L-N-Boc-Ala
15761-38-3

L-N-Boc-Ala

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C45H81N3O16

C45H81N3O16

Conditions
ConditionsYield
With dicyclohexyl-carbodiimide In dichloromethane at 20℃; for 3h;70%
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C37H66N2O12

C37H66N2O12

Conditions
ConditionsYield
Stage #1: (9-E)-deoxo-9-hydroximinoerythromycin A With sodium hydrogencarbonate; p-toluenesulfonyl chloride In dichloromethane; water at 0 - 5℃; for 3h;
Stage #2: With acetic acid In dichloromethane; water for 0.25h; pH=5.3 - 5.5;
Stage #3: With sodium hydroxide In water pH=12 - 12.5; Product distribution / selectivity;
70%
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

N-(Benzyloxycarbonyl)glycine
1138-80-3

N-(Benzyloxycarbonyl)glycine

C47H77N3O16

C47H77N3O16

Conditions
ConditionsYield
With dicyclohexyl-carbodiimide In dichloromethane at 20℃; for 3h;65%
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

erythromycin A 6,9-imino ether

erythromycin A 6,9-imino ether

Conditions
ConditionsYield
With sodium hydrogencarbonate; p-toluenesulfonyl chloride In water; acetone at -5 - 30℃; for 4.5h;55.2%
N-tert-butoxycarbonyl-L-leucine
13139-15-6

N-tert-butoxycarbonyl-L-leucine

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C48H87N3O16

C48H87N3O16

Conditions
ConditionsYield
With dicyclohexyl-carbodiimide In dichloromethane at 20℃; for 3h;53.1%
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

4-methoxybenzoic acid
100-09-4

4-methoxybenzoic acid

C45H74N2O15

C45H74N2O15

Conditions
ConditionsYield
With dicyclohexyl-carbodiimide In dichloromethane at 20℃; for 3h;51.2%
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

9-deoxo-11-deoxy-9,11-epoxy-9-nitroso-3'-des-N-methylerythromycin A
121238-13-9

9-deoxo-11-deoxy-9,11-epoxy-9-nitroso-3'-des-N-methylerythromycin A

Conditions
ConditionsYield
With N-Bromosuccinimide; sodium hydrogencarbonate In 1,2-dimethoxyethane; water for 2h; Ambient temperature;42%
UDP-glucose
133-89-1

UDP-glucose

(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

2'-[O-(β-D-glucopyranosyl)]erythromycin A oxime

2'-[O-(β-D-glucopyranosyl)]erythromycin A oxime

Conditions
ConditionsYield
With magnesium(II) glycosylation by cell extract of Streptomyces hygroscopius ATCC 31080; pH 6.0-9.5;50 mg
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

epichlorohydrin
106-89-8

epichlorohydrin

erythromycin-9-[O-(2,3-epoxypropyl)]oxime
93488-70-1

erythromycin-9-[O-(2,3-epoxypropyl)]oxime

Conditions
ConditionsYield
With potassium carbonate In acetone for 7h; Heating;
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

2-(((benzyloxy)carbonyl)amino)ethyl 1-methanesulfonate
134307-72-5

2-(((benzyloxy)carbonyl)amino)ethyl 1-methanesulfonate

A

C47H79N3O15
256420-10-7

C47H79N3O15

B

C47H79N3O15

C47H79N3O15

Conditions
ConditionsYield
With potassium carbonate In acetone for 24h; Heating;
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

N-(benzyloxycarbonyl)-3-amino-1-propyl methanesulfonate
174626-34-7

N-(benzyloxycarbonyl)-3-amino-1-propyl methanesulfonate

A

C48H81N3O15
883739-43-3

C48H81N3O15

B

C48H81N3O15

C48H81N3O15

Conditions
ConditionsYield
With potassium carbonate In acetone for 24h; Heating;
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

N-(benzyloxycarbonyl)-6-aminohexyl methanesulfonate
75937-26-7

N-(benzyloxycarbonyl)-6-aminohexyl methanesulfonate

A

C51H87N3O15

C51H87N3O15

B

C51H87N3O15

C51H87N3O15

Conditions
ConditionsYield
With potassium carbonate In acetone for 24h; Heating;
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

6-(4-dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyl-tetrahydro-pyran-2-yloxy)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione 10-[O-(2-amino-ethyl)-oxime]
134833-89-9

6-(4-dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyl-tetrahydro-pyran-2-yloxy)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione 10-[O-(2-amino-ethyl)-oxime]

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

6-(4-dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyl-tetrahydro-pyran-2-yloxy)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione 10-[O-(3-amino-propyl)-oxime]
883739-48-8

6-(4-dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyl-tetrahydro-pyran-2-yloxy)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione 10-[O-(3-amino-propyl)-oxime]

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

6-(4-dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyl-tetrahydro-pyran-2-yloxy)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione 10-[O-(6-amino-hexyl)-oxime]
883739-49-9

6-(4-dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-7,12,13-trihydroxy-4-(5-hydroxy-4-methoxy-4,6-dimethyl-tetrahydro-pyran-2-yloxy)-3,5,7,9,11,13-hexamethyl-oxacyclotetradecane-2,10-dione 10-[O-(6-amino-hexyl)-oxime]

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C50H86N6O18

C50H86N6O18

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
3: CH2Cl2; dimethylformamide / 20 °C
4: HF-pyridine / tetrahydrofuran / 0 - 4 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C51H88N6O18

C51H88N6O18

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
3: CH2Cl2; dimethylformamide / 20 °C
4: HF-pyridine / tetrahydrofuran / 0 - 4 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C54H94N6O18

C54H94N6O18

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
3: CH2Cl2; dimethylformamide / 20 °C
4: HF-pyridine / tetrahydrofuran / 0 - 4 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C56H100N6O18Si
883739-50-2

C56H100N6O18Si

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
3: CH2Cl2; dimethylformamide / 20 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C57H102N6O18Si
883739-51-3

C57H102N6O18Si

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
3: CH2Cl2; dimethylformamide / 20 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

C60H108N6O18Si
883739-52-4

C60H108N6O18Si

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: K2CO3 / acetone / 24 h / Heating
2: 100 percent / H2 / Pd/C / methanol / 20 °C
3: CH2Cl2; dimethylformamide / 20 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

A

3-O-descladinosyl-3-OH-6-O-allyl-erythromycin A 9-oxime
722495-12-7

3-O-descladinosyl-3-OH-6-O-allyl-erythromycin A 9-oxime

B

3-halide-4-methyl-thiophene

3-halide-4-methyl-thiophene

Conditions
ConditionsYield
Multi-step reaction with 4 steps
1.1: 71 percent / pyridine hydrochloride / CH2Cl2 / 42 h / 20 °C
2.1: 90 percent / dimethylaminopyridine / pyridine / 3 h / 20 °C
3.1: 56 percent / potassium tert-butoxide / dimethylsulfoxide; tetrahydrofuran / 4 h
4.1: HCl / ethanol; H2O / 6 h / 50 °C
4.2: 72 percent / K2CO3 / methanol / 12 h / 50 °C
View Scheme
(9-E)-deoxo-9-hydroximinoerythromycin A
13127-18-9

(9-E)-deoxo-9-hydroximinoerythromycin A

(3R,4S,5S,6R,7R,9R,11S,12R,13S,14R)-6-((2S,3R,4S,6R)-4-Dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-4,12,13-trihydroxy-3,5,7,9,11,13-hexamethyl-7-[(E)-3-(4-methyl-thiophen-3-yl)-allyloxy]-oxacyclotetradecane-2,10-dione 10-oxime

(3R,4S,5S,6R,7R,9R,11S,12R,13S,14R)-6-((2S,3R,4S,6R)-4-Dimethylamino-3-hydroxy-6-methyl-tetrahydro-pyran-2-yloxy)-14-ethyl-4,12,13-trihydroxy-3,5,7,9,11,13-hexamethyl-7-[(E)-3-(4-methyl-thiophen-3-yl)-allyloxy]-oxacyclotetradecane-2,10-dione 10-oxime

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: 71 percent / pyridine hydrochloride / CH2Cl2 / 42 h / 20 °C
2.1: 90 percent / dimethylaminopyridine / pyridine / 3 h / 20 °C
3.1: 56 percent / potassium tert-butoxide / dimethylsulfoxide; tetrahydrofuran / 4 h
4.1: HCl / ethanol; H2O / 6 h / 50 °C
4.2: 72 percent / K2CO3 / methanol / 12 h / 50 °C
5.1: triethylamine / palladium (II) acetate; triphenylphosphine / acetonitrile / 16 h / Heating
View Scheme

13127-18-9Relevant articles and documents

Translactonization of erythromycin a during oximation: Mixture analysis and reaction monitoring by NMR

Grover, Rajesh K.,Joshi,Batra,Roy, Raja,Bhaduri

, p. 355 - 360 (2001)

Oximation of erythromycin A with hydroxylamine hydrochloride and sodium acetate in methanol led to the formation of pseudoerythromycin A enol ether with erythromycin A oxime as analysed by detailed two-dimensional NMR spectroscopy in the mixture along with traces of 8,9-anhydroerythromycin A 6,9-hemiketal and erythromycin A 6,9:9,12-spiroketal. The formation of the degraded products was established by performing in situ 13C NMR spectroscopy. The analysis suggests that pseudoerythromycin A enol ether is formed by the translactonization of erythromycin A enol ether which forms as a result of acid degradation. Copyright

Synthesis of two and antibacterial activity of one novel oxime ether derivatives of erythromycin A

Dondas,Yaktubay

, p. 1011 - 1015 (2003)

The synthesis of novel erythromycin A 9-O-(2-ethenesulfony-ethyl)-oxime and erythromycin A 9-O-(3-oxo-butyl)-oxime from erythromycin A (EA) by the Michael reaction is described and to describe the effects of transformation of ketone in position 9 of EA to an oxime ether. This transformation occurred in a single step without protecting of any functional moiety of erythromycin oxime and zero waste manner in good yield. The antibacterial screen of EA 9-O-(2-ethenesulfony-ethyl)-oxime is also reported.

Synthetic method of isotope-labeled erythromycylamine

-

Paragraph 0020; 0025-0027; 0033-0035; 0041-0043, (2020/07/28)

The invention discloses a synthetic method of isotope-labeled erythromycylamine, belongs to the field of drug metabolism, and provides a synthetic method which is reasonable in process design, strongin operability and high in yield, can efficiently convert isotope-labeled raw materials into labeled target products, and can realize industrial production of isotope-labeled erythromycylamine. The method takes 13CD3 labeled methyl iodide as a starting raw material, the isotope-labeled erythromycylamine is synthesized by six steps of reactions, optimal preparation steps and reaction conditions arescreened out through a large number of experiments, the whole process is reasonable in design and high in operability, the labeled raw materials can be efficiently converted into labeled target products, the chemical purity of the labeled erythromycylamine prepared through the method can reach 98.5% or above, and the labeled isotope abundance is larger than 98.5%.

Macrolide derivative and application thereof

-

Paragraph 0022; 0045, (2017/08/28)

The invention provides a macrolide derivative of a novel structure. Experiments show that the macrolide derivative has a good promoting effect on alimentary motility and is capable of enhancing intestine peristalsis, increasing defecation quantity and accelerating passing of intestinal content; on such basis, it is further discovered that the macrolide derivative is low in antibiotic activity and small in side effect and can be taken as a gastrointestinal motility promoting drug. Particularly, a compound III-3 screened with the optimal efficacy is subjected to further efficacy evaluation as well as acute toxicity and cardiotoxicity evaluation by domestic rabbits, beagles and marmosets. Experiments show that the compound III-3 is safe and capable of effectively promoting gastrointestinal motility, thereby being excellent in druggability.

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